Publications

Highlighted Publications

Rewiring cancer drivers to activate apoptosis

Nature. 2023 Aug;620(7973):417-425. doi: 10.1038/s41586-023-06348-2.

Abstract: Genes that drive the proliferation, survival, invasion and metastasis of malignant cells have been identified for many human cancers1-4. Independent studies have identified cell death pathways that eliminate cells for the good of the organism5,6. The coexistence of cell death pathways with driver mutations suggests that the cancer driver could be rewired to activate cell death using chemical inducers of proximity (CIPs). Here we describe a new class of molecules called transcriptional/epigenetic CIPs (TCIPs) that recruit the endogenous cancer driver, or a downstream transcription factor, to the promoters of cell death genes, thereby activating their expression. We focused on diffuse large B cell lymphoma, in which the transcription factor B cell lymphoma 6 (BCL6) is deregulated7. BCL6 binds to the promoters of cell death genes and epigenetically suppresses their expression8. We produced TCIPs by covalently linking small molecules that bind BCL6 to those that bind to transcriptional activators that contribute to the oncogenic program, such as BRD4. The most potent molecule, TCIP1, increases binding of BRD4 by 50% over genomic BCL6-binding sites to produce transcriptional elongation at pro-apoptotic target genes within 15 min, while reducing binding of BRD4 over enhancers by only 10%, reflecting a gain-of-function mechanism. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines, at EC50 of 1-10 nM in 72 h and exhibits cell-specific and tissue-specific effects, capturing the combinatorial specificity inherent to transcription. The TCIP concept also has therapeutic applications in regulating the expression of genes for regenerative medicine and developmental disorders.

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Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry

J Am Chem Soc. 2023 Oct 11;145(40):21937-21944. doi: 10.1021/jacs.3c06622.

Abstract: Targeted protein degradation relies on small molecules that induce new protein-protein interactions between targets and the cellular protein degradation machinery. Most of these small molecules feature specific ligands for ubiquitin ligases. Recently, the attachment of cysteine-reactive chemical groups to pre-existing small molecule inhibitors has been shown to drive specific target degradation. We demonstrate here that different cysteine-reactive groups can specify target degradation via distinct ubiquitin ligases. By focusing on the bromodomain ligand JQ1, we identify cysteine-reactive functional groups that drive BRD4 degradation by either DCAF16 or DCAF11. Unlike proteolysis-targeting chimeric molecules (PROTACs), the new compounds use a single small molecule ligand with a well-positioned cysteine-reactive group to induce protein degradation. The finding that nearly identical compounds can engage multiple ubiquitination pathways suggests that targeting cellular pathways that search for and eliminate chemically reactive proteins is a feasible avenue for converting existing small molecule drugs into protein degrader molecules.

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Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality

ACS Cent Sci. 2024 Feb 26;10(6):1156-1166. doi: 10.1021/acscentsci.3c01245.

Abstract: A systematic strategy to develop dual-warhead inhibitors is introduced to circumvent the limitations of conventional covalent inhibitors such as vulnerability to mutations of the corresponding nucleophilic residue. Currently, all FDA-approved covalent small molecules feature one electrophile, leaving open a facile route to acquired resistance. We conducted a systematic analysis of human proteins in the protein data bank to reveal ∼400 unique targets amendable to dual covalent inhibitors, which we term “molecular bidents”. We demonstrated this strategy by targeting two kinases: MKK7 and EGFR. The designed compounds, ZNL-8162 and ZNL-0056, are ATP-competitive inhibitors that form two covalent bonds with cysteines and retain potency against single cysteine mutants. Therefore, molecular bidents represent a new pharmacological modality with the potential for improved selectivity, potency, and drug resistance profile.

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Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

Cell. 2020 Dec 10;183(6):1714-1731.e10. doi: 10.1016/j.cell.2020.10.038.

Abstract: Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-dependent degradation of proteins. TPD is of interest in drug development, as it can address previously inaccessible targets. However, degrader discovery and optimization remains an inefficient process due to a lack of understanding of the relative importance of the key molecular events required to induce target degradation. Here, we use chemo-proteomics to annotate the degradable kinome. Our expansive dataset provides chemical leads for ∼200 kinases and demonstrates that the current practice of starting from the highest potency binder is an ineffective method for discovering active compounds. We develop multitargeted degraders to answer fundamental questions about the ubiquitin proteasome system, uncovering that kinase degradation is p97 dependent. This work will not only fuel kinase degrader discovery, but also provides a blueprint for evaluating targeted degradation across entire gene families to accelerate understanding of TPD beyond the kinome.

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Identification of a potent and selective covalent Pin1 inhibitor.

Nat Chem Biol. 2020 Jun 1. doi: 10.1038/s41589-020-0550-9.

Abstract: Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly overexpressed in human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is dispensable for viability in mice, it is required for activated Ras to induce tumorigenesis, suggesting a role for Pin1 inhibitors in Ras-driven tumors, such as PDAC. We report the development of rationally designed peptide inhibitors that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site. The inhibitors were iteratively optimized for potency, selectivity and cell permeability to give BJP-06-005-3, a versatile tool compound with which to probe Pin1 biology and interrogate its role in cancer. In parallel to inhibitor development, we employed genetic and chemical-genetic strategies to assess the consequences of Pin1 loss in human PDAC cell lines. We demonstrate that Pin1 cooperates with mutant KRAS to promote transformation in PDAC, and that Pin1 inhibition impairs cell viability over time in PDAC cell lines.

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Targeting wild-type and T315I Bcr-Abl by combining allosteric with ATP-site inhibitors.

Nature. 2010;463(7280):501-6.

Abstract: In an effort to find new pharmacological modalities to overcome resistance to ATP-binding-site inhibitors of Bcr-Abl, we recently reported the discovery of GNF-2, a selective allosteric Bcr-Abl inhibitor. Here, using solution NMR, X-ray crystallography, mutagenesis and hydrogen exchange mass spectrometry, we show that GNF-2 binds to the myristate-binding site of Abl, leading to changes in the structural dynamics of the ATP-binding site. GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, when used in combination with the ATP-competitive inhibitors imatinib or nilotinib, suppressed the emergence of resistance mutations in vitro, displayed additive inhibitory activity in biochemical and cellular assays against T315I mutant human Bcr-Abl and displayed in vivo efficacy against this recalcitrant mutant in a murine bone-marrow transplantation model. These results show that therapeutically relevant inhibition of Bcr-Abl activity can be achieved with inhibitors that bind to the myristate-binding site and that combining allosteric and ATP-competitive inhibitors can overcome resistance to either agent alone.

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Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Nature. 2009;462(7276):1070-4

Abstract: The clinical efficacy of epidermal growth factor receptor (EGFR) kinase inhibitors in EGFR-mutant non-small-cell lung cancer (NSCLC) is limited by the development of drug-resistance mutations, including the gatekeeper T790M mutation. Strategies targeting EGFR T790M with irreversible inhibitors have had limited success and are associated with toxicity due to concurrent inhibition of wild-type EGFR. All current EGFR inhibitors possess a structurally related quinazoline-based core scaffold and were identified as ATP-competitive inhibitors of wild-type EGFR. Here we identify a covalent pyrimidine EGFR inhibitor by screening an irreversible kinase inhibitor library specifically against EGFR T790M. These agents are 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors in vitro. They are also effective in murine models of lung cancer driven by EGFR T790M. Co-crystallization studies reveal a structural basis for the increased potency and mutant selectivity of these agents. These mutant-selective irreversible EGFR kinase inhibitors may be clinically more effective and better tolerated than quinazoline-based inhibitors. Our findings demonstrate that functional pharmacological screens against clinically important mutant kinases represent a powerful strategy to identify new classes of mutant-selective kinase inhibitors.

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An ATP-competitive mTOR inhibitor reveals rapamycin-insensitive functions of mTORC1.

J Biol Chem. 2009;284(12)8023-32.

Abstract: The mammalian target of rapamycin (mTOR) kinase is the catalytic subunit of two functionally distinct complexes, mTORC1 and mTORC2, that coordinately promote cell growth, proliferation, and survival. Rapamycin is a potent allosteric mTORC1 inhibitor with clinical applications as an immunosuppressant and anti-cancer agent. Here we find that Torin1, a highly potent and selective ATP-competitive mTOR inhibitor that directly inhibits both complexes, impairs cell growth and proliferation to a far greater degree than rapamycin. Surprisingly, these effects are independent of mTORC2 inhibition and are instead because of suppression of rapamycin-resistant functions of mTORC1 that are necessary for cap-dependent translation and suppression of autophagy. These effects are at least partly mediated by mTORC1-dependent and rapamycin-resistant phosphorylation of 4E-BP1. Our findings challenge the assumption that rapamycin completely inhibits mTORC1 and indicate that direct inhibitors of mTORC1 kinase activity may be more successful than rapamycin at inhibiting tumors that depend on mTORC1.

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2024

Ji W, Du G, Jiang J, Lu W, Mills CE, Yuan L, Jiang F, He Z, Bradshaw GA, Chung M, Jiang Z, Byun WS, Hinshaw SM, Zhang T, Gray NS. Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7) Eur J Med Chem. 2024 Jun 27;276:116613. doi: 10.1016/j.ejmech.2024.116613. Online ahead of print.
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Li Z, Jiang J, Ficarro SB, Beyett TS, To C, Tavares I, Zhu Y, Li J, Eck MJ, Jänne PA, Marto JA, Zhang T, Che J, Gray NS. Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality ACS Cent Sci. 2024 Feb 26;10(6):1156-1166. doi: 10.1021/acscentsci.3c01245. eCollection 2024 Jun 26.
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Chen C, Jiang YP, You I, Gray NS, Lin RZ. Down-Regulation of AKT Proteins Slows the Growth of Mutant-KRAS Pancreatic Tumors Cells. 2024 Jun 19;13(12):1061. doi: 10.3390/cells13121061.
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Liu HY, Li Z, Reindl T, He Z, Qiu X, Golden RP, Donovan KA, Bailey A, Fischer ES, Zhang T, Gray NS, Yang PL. Broad-spectrum activity against mosquito-borne flaviviruses achieved by a targeted protein degradation mechanism Nat Commun. 2024 Jun 19;15(1):5179. doi: 10.1038/s41467-024-49161-9.
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Li Z, Liu HY, He Z, Chakravarty A, Golden RP, Jiang Z, You I, Yue H, Donovan KA, Du G, Che J, Tse J, Che I, Lu W, Fischer ES, Zhang T, Gray NS, Yang PL. Discovery of Potent Degraders of the Dengue Virus Envelope Protein bioRxiv [Preprint]. 2024 Jun 2:2024.06.01.596987. doi: 10.1101/2024.06.01.596987.
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Martin TD, Watson EV, Choi MY, Nabet B, Gray NS, Xu Q, Elledge SJ. Proteasomal control of anti-CRISPRs for the regulation of CRISPR/Cas9 activity using Cas9-ACROBAT bioRxiv [Preprint]. 2024 May 13:2024.05.13.593596. doi: 10.1101/2024.05.13.593596.
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Razumkov H, Jiang Z, Baek K, You I, Geng Q, Donovan KA, Tang MT, Metivier RJ, Mageed N, Seo P, Li Z, Byun WS, Hinshaw SM, Sarott RC, Fischer ES, Gray NS. Discovery of CRBN-dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library bioRxiv [Preprint]. 2024 May 5:2024.05.04.592550. doi: 10.1101/2024.05.04.592550.
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Radko-Juettner S, Yue H, Myers JA, Carter RD, Robertson AN, Mittal P, Zhu Z, Hansen BS, Donovan KA, Hunkeler M, Rosikiewicz W, Wu Z, McReynolds MG, Roy Burman SS, Schmoker AM, Mageed N, Brown SA, Mobley RJ, Partridge JF, Stewart EA, Pruett-Miller SM, Nabet B, Peng J, Gray NS, Fischer ES, Roberts CWM. Author Correction: Targeting DCAF5 suppresses SMARCB1-mutant cancer by stabilizing SWI/SNF Nature. 2024 May;629(8012):E12. doi: 10.1038/s41586-024-07402-3.
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Ke S, Dang F, Wang L, Chen JY, Naik MT, Li W, Thavamani A, Kim N, Naik NM, Sui H, Tang W, Qiu C, Koikawa K, Batalini F, Stern Gatof E, Isaza DA, Patel JM, Wang X, Clohessy JG, Heng YJ, Lahav G, Liu Y, Gray NS, Zhou XZ, Wei W, Wulf GM, Lu KP. Reciprocal antagonism of PIN1-APC/C(CDH1) governs mitotic protein stability and cell cycle entry Nat Commun. 2024 Apr 15;15(1):3220. doi: 10.1038/s41467-024-47427-w.
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Radko-Juettner S, Yue H, Myers JA, Carter RD, Robertson AN, Mittal P, Zhu Z, Hansen BS, Donovan KA, Hunkeler M, Rosikiewicz W, Wu Z, McReynolds MG, Roy Burman SS, Schmoker AM, Mageed N, Brown SA, Mobley RJ, Partridge JF, Stewart EA, Pruett-Miller SM, Nabet B, Peng J, Gray NS, Fischer ES, Roberts CWM. Targeting DCAF5 suppresses SMARCB1-mutant cancer by stabilizing SWI/SNF Nature. 2024 Apr;628(8007):442-449. doi: 10.1038/s41586-024-07250-1. Epub 2024 Mar 27.
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Lantermans HC, Ma F, Kuil A, van Kesteren S, Yasinoglu S, Yang G, Buhrlage SJ, Wang J, Gray NS, Kersten MJ, Treon SP, Pals ST, Spaargaren M. The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma Leukemia. 2024 Jul;38(7):1570-1580. doi: 10.1038/s41375-024-02207-9. Epub 2024 Mar 7.
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Erickson EC, You I, Perry G, Dugourd A, Donovan KA, Crafter C, Johannes JW, Williamson S, Moss JI, Ros S, Ziegler RE, Barry ST, Fischer ES, Gray NS, Madsen RR, Toker A. Multiomic profiling of breast cancer cells uncovers stress MAPK-associated sensitivity to AKT degradation Sci Signal. 2024 Feb 27;17(825):eadf2670. doi: 10.1126/scisignal.adf2670. Epub 2024 Feb 27.
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Li Z, Lu W, Beyett TS, Ficarro SB, Jiang J, Tse J, Kim AY, Marto JA, Che J, Jänne PA, Eck MJ, Zhang T, Gray NS. ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases J Med Chem. 2024 Feb 22;67(4):2837-2848. doi: 10.1021/acs.jmedchem.3c01891. Epub 2024 Feb 1.
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Wang L, Bohmer MJ, Wang J, Nardella F, Calla J, Laureano De Souza M, Schindler KA, Montejo L, Mittal N, Rocamora F, Treat M, Charlton JT, Tumwebaze PK, Rosenthal PJ, Cooper RA, Chakrabarti R, Winzeler EA, Chakrabarti D, Gray NS. Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases J Med Chem. 2024 Jan 25;67(2):1460-1480. doi: 10.1021/acs.jmedchem.3c02046. Epub 2024 Jan 12.
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2023

Sarott R, Gourisankar S, Karim B, Nettles S, Yang H, Dwyer BG, Simanauskaite JM, Tse J, Abuzaid H, Krokhotin A, Zhang T, Hinshaw SM, Green MR, Crabtree GR, Gray NS. Borrowing Transcriptional Kinases to Activate Apoptosis bioRxiv [Preprint]. 2023 Oct 25:2023.10.23.563687. doi: 10.1101/2023.10.23.563687.
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Hassan MM, Li YD, Ma MW, Teng M, Byun WS, Puvar K, Lumpkin R, Sandoval B, Rutter JC, Jin CY, Wang MY, Xu S, Schmoker AM, Cheong H, Groendyke BJ, Qi J, Fischer ES, Ebert BL, Gray NS. Exploration of the Tunability of BRD4 Degradation by DCAF16 Trans-labelling Covalent Glues bioRxiv [Preprint]. 2023 Oct 10:2023.10.07.561308. doi: 10.1101/2023.10.07.561308.
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Sarott RC, You I, Li YD, Toenjes ST, Donovan KA, Seo P, Ordonez M, Byun WS, Hassan MM, Wachter F, Chouchani ET, Słabicki M, Fischer ES, Ebert BL, Hinshaw SM, Gray NS. Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry J Am Chem Soc. 2023 Oct 11;145(40):21937-21944. doi: 10.1021/jacs.3c06622. Epub 2023 Sep 28.
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Mukhopadhyay S, Huang HY, Lin Z, Ranieri M, Li S, Sahu S, Liu Y, Ban Y, Guidry K, Hu H, Lopez A, Sherman F, Tan YJ, Lee YT, Armstrong AP, Dolgalev I, Sahu P, Zhang T, Lu W, Gray NS, Christensen JG, Tang TT, Velcheti V, Khodadadi-Jamayran A, Wong KK, Neel BG. Genome-Wide CRISPR Screens Identify Multiple Synthetic Lethal Targets That Enhance KRASG12C Inhibitor Efficacy Cancer Res. 2023 Dec 15;83(24):4095-4111. doi: 10.1158/0008-5472.CAN-23-2729.
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Ji W, Byun WS, Lu W, Zhu X, Donovan KA, Dwyer BG, Che J, Yuan L, Abulaiti X, Corsello SM, Fischer ES, Zhang T, Gray NS. Proteomics-Based Discovery of First-in-Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2) Angew Chem Int Ed Engl. 2023 Oct 23;62(43):e202308292. doi: 10.1002/anie.202308292. Epub 2023 Sep 15.
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Gourisankar S, Krokhotin A, Ji W, Liu X, Chang CY, Kim SH, Li Z, Wenderski W, Simanauskaite JM, Yang H, Vogel H, Zhang T, Green MR, Gray NS, Crabtree GR. Author Correction: Rewiring cancer drivers to activate apoptosis Nature. 2023 Sep;621(7977):E27. doi: 10.1038/s41586-023-06543-1.
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Hatcher JM, Zwirek M, Sarhan AR, Vatsan PS, Tonelli F, Alessi DR, Davies P, Gray NS. Development of a highly potent and selective degrader of LRRK2 Bioorg Med Chem Lett. 2023 Oct 1;94:129449. doi: 10.1016/j.bmcl.2023.129449. Epub 2023 Aug 15.
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Kim Y, Seo P, Jeon E, You I, Hwang K, Kim N, Tse J, Bae J, Choi HS, Hinshaw SM, Gray NS, Sim T. Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase Cell Chem Biol. 2023 Nov 16;30(11):1414-1420.e5. doi: 10.1016/j.chembiol.2023.07.008. Epub 2023 Aug 10.
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Gourisankar S, Krokhotin A, Ji W, Liu X, Chang CY, Kim SH, Li Z, Wenderski W, Simanauskaite JM, Yang H, Vogel H, Zhang T, Green MR, Gray NS, Crabtree GR. Rewiring cancer drivers to activate apoptosis Nature. 2023 Aug;620(7973):417-425. doi: 10.1038/s41586-023-06348-2. Epub 2023 Jul 26.
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Teng M, Gray NS. The rise of degrader drugs Cell Chem Biol. 2023 Aug 17;30(8):864-878. doi: 10.1016/j.chembiol.2023.06.020. Epub 2023 Jul 25.
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Arwood ML, Liu Y, Harkins SK, Weinstock DM, Yang L, Stevenson KE, Plana OD, Dong J, Cirka H, Jones KL, Virtanen AT, Gupta DG, Ceas A, Lawney B, Yoda A, Leahy C, Hao M, He Z, Choi HG, Wang Y, Silvennoinen O, Hubbard SR, Zhang T, Gray NS, Li LS. New scaffolds for type II JAK2 inhibitors overcome the acquired G993A resistance mutation Cell Chem Biol. 2023 Jun 15;30(6):618-631.e12. doi: 10.1016/j.chembiol.2023.05.007. Epub 2023 Jun 7.
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de Matos Simoes R, Shirasaki R, Downey-Kopyscinski SL, Matthews GM, Barwick BG, Gupta VA, Dupéré-Richer D, Yamano S, Hu Y, Sheffer M, Dhimolea E, Dashevsky O, Gandolfi S, Ishiguro K, Meyers RM, Bryan JG, Dharia NV, Hengeveld PJ, Brüggenthies JB, Tang H, Aguirre AJ, Sievers QL, Ebert BL, Glassner BJ, Ott CJ, Bradner JE, Kwiatkowski NP, Auclair D, Levy J, Keats JJ, Groen RWJ, Gray NS, Culhane AC, McFarland JM, Dempster JM, Licht JD, Boise LH, Hahn WC, Vazquez F, Tsherniak A, Mitsiades CS. Genome-scale functional genomics identify genes preferentially essential for multiple myeloma cells compared to other neoplasias Nat Cancer. 2023 May;4(5):754-773. doi: 10.1038/s43018-023-00550-x. Epub 2023 May 26.
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Koide E, Mohardt ML, Doctor ZM, Yang A, Hao M, Donovan KA, Kuismi CC, Nelson AJ, Abell K, Aguiar M, Che J, Stokes MP, Zhang T, Aguirre AJ, Fischer ES, Gray NS, Jiang B, Nabet B. Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity Chembiochem. 2023 Oct 4;24(19):e202300141. doi: 10.1002/cbic.202300141. Epub 2023 Jul 24.
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Gao Y, Jiang B, Kim H, Berberich MJ, Che J, Donovan KA, Hatcher JM, Huerta F, Kwiatkowski NP, Liu Y, Liuni PP, Metivier RJ, Murali VK, Nowak RP, Zhang T, Fischer ES, Gray NS, Jones LH. Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions J Med Chem. 2023 Apr 27;66(8):5524-5535. doi: 10.1021/acs.jmedchem.2c01864. Epub 2023 Apr 10.
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Perurena N, Lock R, Davis RA, Raghavan S, Pilla NF, Ng R, Loi P, Guild CJ, Miller AL, Sicinska E, Cleary JM, Rubinson DA, Wolpin BM, Gray NS, Santagata S, Hahn WC, Morton JP, Sansom OJ, Aguirre AJ, Cichowski K. USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities Cell Rep Med. 2023 Apr 18;4(4):101007. doi: 10.1016/j.xcrm.2023.101007. Epub 2023 Apr 7.
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Jiang B, Weinstock DM, Donovan KA, Sun HW, Wolfe A, Amaka S, Donaldson NL, Wu G, Jiang Y, Wilcox RA, Fischer ES, Gray NS, Wu W. ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas Cell Chem Biol. 2023 Apr 20;30(4):383-393.e6. doi: 10.1016/j.chembiol.2023.03.007. Epub 2023 Apr 3.
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Lu W, Fan M, Ji W, Tse J, You I, Ficarro SB, Tavares I, Che J, Kim AY, Zhu X, Boghossian A, Rees MG, Ronan MM, Roth JA, Hinshaw SM, Nabet B, Corsello SM, Kwiatkowski N, Marto JA, Zhang T, Gray NS. Structure-Based Design of Y-Shaped Covalent TEAD Inhibitors J Med Chem. 2023 Apr 13;66(7):4617-4632. doi: 10.1021/acs.jmedchem.2c01548. Epub 2023 Mar 22.
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Wang ES, Gray NS. Shining light on reprogramming Tregs for cancer therapy Cell Chem Biol. 2023 Mar 16;30(3):231-233. doi: 10.1016/j.chembiol.2023.02.009.
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Bohmer MJ, Wang J, Istvan ES, Luth MR, Collins JE, Huttlin EL, Wang L, Mittal N, Hao M, Kwiatkowski NP, Gygi SP, Chakrabarti R, Deng X, Goldberg DE, Winzeler EA, Gray NS, Chakrabarti D. Human Polo-like Kinase Inhibitors as Antiplasmodials ACS Infect Dis. 2023 Apr 14;9(4):1004-1021. doi: 10.1021/acsinfecdis.3c00025. Epub 2023 Mar 15.
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Teng M, Jiang J, Wang ES, Geng Q, Toenjes ST, Donovan KA, Mageed N, Yue H, Nowak RP, Wang J, Manz TD, Fischer ES, Cantley LC, Gray NS. Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader Angew Chem Int Ed Engl. 2023 Apr 24;62(18):e202302364. doi: 10.1002/anie.202302364. Epub 2023 Mar 27.
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Yao Y, Ng JF, Park WD, Samur M, Morelli E, Encinas Mayoral J, Chyra Z, Xu Y, Derebail S, Epstein C, Nabet B, Chesi M, Gray NS, Young RA, Kwiatkowski N, Mitsiades C, Anderson KC, Lin CY, Munshi NC, Fulciniti M. CDK7 controls E2F- and MYC-driven proliferative and metabolic vulnerabilities in multiple myeloma Blood. 2023 Jun 8;141(23):2841-2852. doi: 10.1182/blood.2022018885.
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Lu W, Liu Y, Gao Y, Geng Q, Gurbani D, Li L, Ficarro SB, Meyer CJ, Sinha D, You I, Tse J, He Z, Ji W, Che J, Kim AY, Yu T, Wen K, Anderson KC, Marto JA, Westover KD, Zhang T, Gray NS. Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1 J Med Chem. 2023 Mar 9;66(5):3356-3371. doi: 10.1021/acs.jmedchem.2c01834. Epub 2023 Feb 24.
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Li YD, Ma MW, Hassan MM, Hunkeler M, Teng M, Puvar K, Lumpkin R, Sandoval B, Jin CY, Ficarro SB, Wang MY, Xu S, Groendyke BJ, Sigua LH, Tavares I, Zou C, Tsai JM, Park PMC, Yoon H, Majewski FC, Marto JA, Qi J, Nowak RP, Donovan KA, Słabicki M, Gray NS, Fischer ES, Ebert BL. Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders bioRxiv [Preprint]. 2023 Feb 15:2023.02.14.528208. doi: 10.1101/2023.02.14.528208.
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Darabedian N, Ji W, Fan M, Lin S, Seo HS, Vinogradova EV, Yaron TM, Mills EL, Xiao H, Senkane K, Huntsman EM, Johnson JL, Che J, Cantley LC, Cravatt BF, Dhe-Paganon S, Stegmaier K, Zhang T, Gray NS, Chouchani ET. Depletion of creatine phosphagen energetics with a covalent creatine kinase inhibitor Nat Chem Biol. 2023 Jul;19(7):815-824. doi: 10.1038/s41589-023-01273-x. Epub 2023 Feb 23.
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Zerfas BL, Huerta F, Liu H, Du G, Gray NS, Jones LH, Nowak RP. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells Methods Enzymol. 2023;681:169-188. doi: 10.1016/bs.mie.2022.08.013. Epub 2022 Sep 26.
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Ke S, Dang F, Wang L, Chen JY, Naik MT, Thavamani A, Liu Y, Li W, Kim N, Naik NM, Sui H, Tang W, Qiu C, Koikawa K, Batalini F, Wang X, Clohessy JG, Heng YJ, Lahav G, Gray NS, Zho XZ, Wei W, Wulf GM, Lu KP. Reciprocal inhibition of PIN1 and APC/C(CDH1) controls timely G1/S transition and creates therapeutic vulnerability Res Sq [Preprint]. 2023 Jan 19:rs.3.rs-2447544. doi: 10.21203/rs.3.rs-2447544/v1.
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Lu DY, Ellegast JM, Ross KN, Malone CF, Lin S, Mabe NW, Dharia NV, Meyer A, Conway A, Su AH, Selich-Anderson J, Taslim C, Byrum AK, Seong BKA, Adane B, Gray NS, Rivera MN, Lessnick SL, Stegmaier K. The ETS transcription factor ETV6 constrains the transcriptional activity of EWS-FLI to promote Ewing sarcoma Nat Cell Biol. 2023 Feb;25(2):285-297. doi: 10.1038/s41556-022-01059-8. Epub 2023 Jan 19.
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Ji W, Wang ES, Manz TD, Jiang J, Donovan KA, Abulaiti X, Fischer ES, Cantley LC, Zhang T, Gray NS. Development of potent and selective degraders of PI5P4Kγ Eur J Med Chem. 2023 Feb 5;247:115027. doi: 10.1016/j.ejmech.2022.115027. Epub 2022 Dec 24.
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Malone CF, Kim M, Alexe G, Engel K, Forman AB, Robichaud A, Conway AS, Goodale A, Meyer A, Khalid D, Thayakumar A, Hatcher JM, Gray NS, Piccioni F, Stegmaier K. Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors Cancer Res. 2023 Jan 18;83(2):285-300. doi: 10.1158/0008-5472.CAN-21-4309.
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Boytz R, Słabicki M, Ramaswamy S, Patten JJ, Zou C, Meng C, Hurst BL, Wang J, Nowak RP, Yang PL, Sattler M, Stone RM, Griffin JD, Gray NS, Gummuluru S, Davey RA, Weisberg E. Anti-SARS-CoV-2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID-19 therapy J Med Virol. 2023 Jan;95(1):e28157. doi: 10.1002/jmv.28157. Epub 2022 Sep 28.
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2022

Zerfas BL, Huerta F, Liu H, Du G, Gray NS, Jones LH, Nowak RP. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells Methods Enzymol. 2023;681:169-188. doi: 10.1016/bs.mie.2022.08.013. Epub 2022 Sep 26.
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Ji W, Wang ES, Manz TD, Jiang J, Donovan KA, Abulaiti X, Fischer ES, Cantley LC, Zhang T, Gray NS. Development of potent and selective degraders of PI5P4Kγ Eur J Med Chem. 2023 Feb 5;247:115027. doi: 10.1016/j.ejmech.2022.115027. Epub 2022 Dec 24.
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Zhang J, Pearson AJ, Sabherwal N, Telfer BA, Ali N, Kan K, Xu Q, Zhang W, Chen F, Li S, Wang J, Gray NS, Risa-Ebrí B, Finegan KG, Cross MJ, Giurisato E, Whitmarsh AJ, Tournier C. Inhibiting ERK5 overcomes breast cancer resistance to anti-HER2 therapy by targeting the G1/S cell cycle transition Cancer Res Commun. 2022 Mar 10;2(3):131-145. doi: 10.1158/2767-9764.CRC-21-0089.
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Chow HY, Karchugina S, Groendyke BJ, Toenjes S, Hatcher J, Donovan KA, Fischer ES, Abalakov G, Faezov B, Dunbrack R, Gray NS, Chernoff J. Development and Utility of a PAK1-Selective Degrader J Med Chem. 2022 Dec 8;65(23):15627-15641. doi: 10.1021/acs.jmedchem.2c00756. Epub 2022 Nov 23.
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Fan M, Lu W, Che J, Kwiatkowski NP, Gao Y, Seo HS, Ficarro SB, Gokhale PC, Liu Y, Geffken EA, Lakhani J, Song K, Kuljanin M, Ji W, Jiang J, He Z, Tse J, Boghossian AS, Rees MG, Ronan MM, Roth JA, Mancias JD, Marto JA, Dhe-Paganon S, Zhang T, Gray NS. Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling Elife. 2022 Oct 27;11:e78810. doi: 10.7554/eLife.78810.
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You I, Donovan KA, Krupnick NM, Boghossian AS, Rees MG, Ronan MM, Roth JA, Fischer ES, Wang ES, Gray NS. Acute pharmacological degradation of ERK5 does not inhibit cellular immune response or proliferation Cell Chem Biol. 2022 Nov 17;29(11):1630-1638.e7. doi: 10.1016/j.chembiol.2022.09.004. Epub 2022 Oct 10.
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Cruite JT, Dann GP, Che J, Donovan KA, Ferrao S, Ficarro SB, Fischer ES, Gray NS, Huerta F, Kong NR, Liu H, Marto JA, Metivier RJ, Nowak RP, Zerfas BL, Jones LH. Cereblon covalent modulation through structure-based design of histidine targeting chemical probes RSC Chem Biol. 2022 Jul 8;3(9):1105-1110. doi: 10.1039/d2cb00078d. eCollection 2022 Aug 31.
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Boytz R, Słabicki M, Ramaswamy S, Patten JJ, Zou C, Meng C, Hurst BL, Wang J, Nowak RP, Yang PL, Sattler M, Stone RM, Griffin JD, Gray NS, Gummuluru S, Davey RA, Weisberg E. Anti-SARS-CoV-2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID-19 therapy J Med Virol. 2023 Jan;95(1):e28157. doi: 10.1002/jmv.28157. Epub 2022 Sep 28.
View in: PubMed

Du G, Jiang J, Henning NJ, Safaee N, Koide E, Nowak RP, Donovan KA, Yoon H, You I, Yue H, Eleuteri NA, He Z, Li Z, Huang HT, Che J, Nabet B, Zhang T, Fischer ES, Gray NS. Exploring the target scope of KEAP1 E3 ligase-based PROTACs Cell Chem Biol. 2022 Oct 20;29(10):1470-1481.e31. doi: 10.1016/j.chembiol.2022.08.003. Epub 2022 Sep 6.
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Verano AL, You I, Donovan KA, Mageed N, Yue H, Nowak RP, Fischer ES, Wang ES, Gray NS. Redirecting the Neo-Substrate Specificity of Cereblon-Targeting PROTACs to Helios ACS Chem Biol. 2022 Sep 16;17(9):2404-2410. doi: 10.1021/acschembio.2c00439. Epub 2022 Aug 25.
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Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Retraction Notice to: Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2 Cell. 2022 Aug 4;185(16):3058. doi: 10.1016/j.cell.2022.07.008.
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Hsu A, Duan Q, Day DS, Luo X, McMahon S, Huang Y, Feldman ZB, Jiang Z, Zhang T, Liang Y, Alexanian M, Padmanabhan A, Brown JD, Lin CY, Gray NS, Young RA, Bruneau BG, Haldar SM. Targeting transcription in heart failure via CDK7/12/13 inhibition Nat Commun. 2022 Jul 27;13(1):4345. doi: 10.1038/s41467-022-31541-8.
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Mehta S, Buyanbat A, Kai Y, Karayel O, Goldman SR, Seruggia D, Zhang K, Fujiwara Y, Donovan KA, Zhu Q, Yang H, Nabet B, Gray NS, Mann M, Fischer ES, Adelman K, Orkin SH. Temporal resolution of gene derepression and proteome changes upon PROTAC-mediated degradation of BCL11A protein in erythroid cells Cell Chem Biol. 2022 Aug 18;29(8):1273-1287.e8. doi: 10.1016/j.chembiol.2022.06.007. Epub 2022 Jul 14.
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Zheng Y, Sethi R, Mangala LS, Taylor C, Goldsmith J, Wang M, Masuda K, Carrami EM, Mannion D, Miranda F, Herrero-Gonzalez S, Hellner K, Chen F, Alsaadi A, Albukhari A, Fotso DC, Yau C, Jiang D, Pradeep S, Rodriguez-Aguayo C, Lopez-Berestein G, Knapp S, Gray NS, Campo L, Myers KA, Dhar S, Ferguson D, Bast RC Jr, Sood AK, von Delft F, Ahmed AA. Author Correction: Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation Nat Commun. 2022 Jun 10;13(1):3352. doi: 10.1038/s41467-022-31011-1.
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Teng M, Luskin MR, Cowan-Jacob SW, Ding Q, Fabbro D, Gray NS. The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug J Med Chem. 2022 Jun 9;65(11):7581-7594. doi: 10.1021/acs.jmedchem.2c00373. Epub 2022 May 24.
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Li Z, Ishida R, Liu Y, Wang J, Li Y, Gao Y, Jiang J, Che J, Sheltzer JM, Robers MB, Zhang T, Westover KD, Nabet B, Gray NS. Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold Eur J Med Chem. 2022 Aug 5;238:114433. doi: 10.1016/j.ejmech.2022.114433. Epub 2022 May 8.
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Beyett TS, To C, Heppner DE, Rana JK, Schmoker AM, Jang J, De Clercq DJH, Gomez G, Scott DA, Gray NS, Jänne PA, Eck MJ. Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors Nat Commun. 2022 May 9;13(1):2530. doi: 10.1038/s41467-022-30258-y.
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Powell CE, Hatcher JM, Jiang J, Vatsan PS, Che J, Gray NS. Selective Macrocyclic Inhibitors of DYRK1A/B ACS Med Chem Lett. 2022 Mar 8;13(4):577-585. doi: 10.1021/acsmedchemlett.1c00630. eCollection 2022 Apr 14.
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Li X, Huang CH, Sánchez-Rivera FJ, Kennedy MC, Tschaharganeh DF, Morris JP 4th, Montinaro A, O’Rourke KP, Banito A, Wilkinson JE, Chen CC, Ho YJ, Dow LE, Tian S, Luan W, de Stanchina E, Zhang T, Gray NS, Walczak H, Lowe SW. A preclinical platform for assessing antitumor effects and systemic toxicities of cancer drug targets Proc Natl Acad Sci U S A. 2022 Apr 26;119(17):e2110557119. doi: 10.1073/pnas.2110557119. Epub 2022 Apr 20.
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To C, Beyett TS, Jang J, Feng WW, Bahcall M, Haikala HM, Shin BH, Heppner DE, Rana JK, Leeper BA, Soroko KM, Poitras MJ, Gokhale PC, Kobayashi Y, Wahid K, Kurppa KJ, Gero TW, Cameron MD, Ogino A, Mushajiang M, Xu C, Zhang Y, Scott DA, Eck MJ, Gray NS, Jänne PA. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer Nat Cancer. 2022 Apr;3(4):402-417. doi: 10.1038/s43018-022-00351-8. Epub 2022 Apr 14.
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Ellegast JM, Alexe G, Hamze A, Lin S, Uckelmann HJ, Rauch PJ, Pimkin M, Ross LS, Dharia NV, Robichaud AL, Conway AS, Khalid D, Perry JA, Wunderlich M, Benajiba L, Pikman Y, Nabet B, Gray NS, Orkin SH, Stegmaier K. Unleashing Cell-Intrinsic Inflammation as a Strategy to Kill AML Blasts Cancer Discov. 2022 Jul 6;12(7):1760-1781. doi: 10.1158/2159-8290.CD-21-0956.
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Gero TW, Heppner DE, Beyett TS, To C, Azevedo SC, Jang J, Bunnell T, Feru F, Li Z, Shin BH, Soroko KM, Gokhale PC, Gray NS, Jänne PA, Eck MJ, Scott DA. Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC Bioorg Med Chem Lett. 2022 Jul 15;68:128718. doi: 10.1016/j.bmcl.2022.128718. Epub 2022 Apr 1.
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Silva MC, Nandi G, Donovan KA, Cai Q, Berry BC, Nowak RP, Fischer ES, Gray NS, Ferguson FM, Haggarty SJ. Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy Front Cell Neurosci. 2022 Mar 3;16:801179. doi: 10.3389/fncel.2022.801179. eCollection 2022.
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Munshi M, Liu X, Kofides A, Tsakmaklis N, Guerrera ML, Hunter ZR, Palomba ML, Argyropoulos KV, Patterson CJ, Canning AG, Meid K, Gustine J, Branagan AR, Flynn CA, Sarosiek S, Castillo JJ, Wang J, Buhrlage SJ, Gray NS, Munshi NC, Anderson KC, Treon SP, Yang G. A new role for the SRC family kinase HCK as a driver of SYK activation in MYD88 mutated lymphomas Blood Adv. 2022 Jun 14;6(11):3332-3338. doi: 10.1182/bloodadvances.2021006147.
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Gao Y, Volegova M, Nasholm N, Das S, Kwiatkowski N, Abraham BJ, Zhang T, Gray NS, Gustafson C, Krajewska M, George RE. Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma Front Oncol. 2022 Jan 27;11:773186. doi: 10.3389/fonc.2021.773186. eCollection 2021.
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Son J, Jang J, Beyett TS, Eum Y, Haikala HM, Verano A, Lin M, Hatcher JM, Kwiatkowski NP, Eser PÖ, Poitras MJ, Wang S, Xu M, Gokhale PC, Cameron MD, Eck MJ, Gray NS, Jänne PA. A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer Cancer Res. 2022 Apr 15;82(8):1633-1645. doi: 10.1158/0008-5472.CAN-21-2693.
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Ryu S, Park JE, Ham YJ, Lim DC, Kwiatkowski NP, Kim DH, Bhunia D, Kim ND, Yaffe MB, Son W, Kim N, Choi TI, Swain P, Kim CH, Lee JY, Gray NS, Lee KS, Sim T. Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1 J Med Chem. 2022 Feb 10;65(3):1915-1932. doi: 10.1021/acs.jmedchem.1c01359. Epub 2022 Jan 14.
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Teng M, Lu W, Donovan KA, Sun J, Krupnick NM, Nowak RP, Li YD, Sperling AS, Zhang T, Ebert BL, Fischer ES, Gray NS. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216 J Med Chem. 2022 Jan 13;65(1):747-756. doi: 10.1021/acs.jmedchem.1c01832. Epub 2021 Dec 29.
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Vervoort SJ, Devlin JR, Kwiatkowski N, Teng M, Gray NS, Johnstone RW. Targeting transcription cycles in cancer Nat Rev Cancer. 2022 Jan;22(1):5-24. doi: 10.1038/s41568-021-00411-8. Epub 2021 Oct 21.
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Li Q, Jiang B, Guo J, Shao H, Del Priore IS, Chang Q, Kudo R, Li Z, Razavi P, Liu B, Boghossian AS, Rees MG, Ronan MM, Roth JA, Donovan KA, Palafox M, Reis-Filho JS, de Stanchina E, Fischer ES, Rosen N, Serra V, Koff A, Chodera JD, Gray NS, Chandarlapaty S. INK4 Tumor Suppressor Proteins Mediate Resistance to CDK4/6 Kinase Inhibitors Cancer Discov. 2022 Feb;12(2):356-371. doi: 10.1158/2159-8290.CD-20-1726. Epub 2021 Sep 20.
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2021

Gao Y, Volegova M, Nasholm N, Das S, Kwiatkowski N, Abraham BJ, Zhang T, Gray NS, Gustafson C, Krajewska M, George RE. Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma Front Oncol. 2022 Jan 27;11:773186. doi: 10.3389/fonc.2021.773186. eCollection 2021.
View in: PubMed

Teng M, Lu W, Donovan KA, Sun J, Krupnick NM, Nowak RP, Li YD, Sperling AS, Zhang T, Ebert BL, Fischer ES, Gray NS. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216 J Med Chem. 2022 Jan 13;65(1):747-756. doi: 10.1021/acs.jmedchem.1c01832. Epub 2021 Dec 29.
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Privalsky TM, Soohoo AM, Wang J, Walsh CT, Wright GD, Gordon EM, Gray NS, Khosla C. Prospects for Antibacterial Discovery and Development J Am Chem Soc. 2021 Dec 22;143(50):21127-21142. doi: 10.1021/jacs.1c10200. Epub 2021 Dec 3.
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Hatcher JM, Vatsan PS, Wang E, Jiang J, Gray NS. Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19 ACS Med Chem Lett. 2021 Oct 22;12(11):1689-1693. doi: 10.1021/acsmedchemlett.1c00300. eCollection 2021 Nov 11.
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Kaltheuner IH, Anand K, Moecking J, Düster R, Wang J, Gray NS, Geyer M. Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation Nat Commun. 2021 Nov 16;12(1):6607. doi: 10.1038/s41467-021-26935-z.
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Vervoort SJ, Devlin JR, Kwiatkowski N, Teng M, Gray NS, Johnstone RW. Targeting transcription cycles in cancer Nat Rev Cancer. 2022 Jan;22(1):5-24. doi: 10.1038/s41568-021-00411-8. Epub 2021 Oct 21.
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Zhu H, Ficarro SB, Alexander WM, Fleming LE, Adelmant G, Zhang T, Willetts M, Decker J, Brehmer S, Krause M, East MP, Gray NS, Johnson GL, Kruppa G, Marto JA. PRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors Anal Chem. 2021 Oct 19;93(41):13791-13799. doi: 10.1021/acs.analchem.1c02349. Epub 2021 Oct 4.
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Li Q, Jiang B, Guo J, Shao H, Del Priore IS, Chang Q, Kudo R, Li Z, Razavi P, Liu B, Boghossian AS, Rees MG, Ronan MM, Roth JA, Donovan KA, Palafox M, Reis-Filho JS, de Stanchina E, Fischer ES, Rosen N, Serra V, Koff A, Chodera JD, Gray NS, Chandarlapaty S. INK4 Tumor Suppressor Proteins Mediate Resistance to CDK4/6 Kinase Inhibitors Cancer Discov. 2022 Feb;12(2):356-371. doi: 10.1158/2159-8290.CD-20-1726. Epub 2021 Sep 20.
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Lu W, Kostic M, Zhang T, Che J, Patricelli MP, Jones LH, Chouchani ET, Gray NS. Correction: Fragment-based covalent ligand discovery RSC Chem Biol. 2021 Feb 22;2(2):670-671. doi: 10.1039/d1cb90008k. eCollection 2021 Apr 1.
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Lu W, Kostic M, Zhang T, Che J, Patricelli MP, Jones LH, Chouchani ET, Gray NS. Fragment-based covalent ligand discovery RSC Chem Biol. 2021 Feb 9;2(2):354-367. doi: 10.1039/d0cb00222d. eCollection 2021 Apr 1.
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Powell CE, Du G, Bushman JW, He Z, Zhang T, Fischer ES, Gray NS. Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC Med Chem. 2021 Jul 6;12(8):1381-1390.
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Teng M, Jiang J, Ficarro SB, Seo HS, Bae JH, Donovan KA, Fischer ES, Zhang T, Dhe-Paganon S, Marto JA, Gray NS. Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 2021 Jul 21;12(8):1302-1307.
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Koikawa K, Kibe S, Suizu F, Sekino N, Kim N, Manz TD, Pinch BJ, Akshinthala D, Verma A, Gaglia G, Nezu Y, Ke S, Qiu C, Ohuchida K, Oda Y, Lee TH, Wegiel B, Clohessy JG, London N, Santagata S, Wulf GM, Hidalgo M, Muthuswamy SK, Nakamura M, Gray NS, Zhou XZ, Lu KP. Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy. Cell. 2021 Aug 6.
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Seong BKA, Dharia NV, Lin S, Donovan KA, Chong S, Robichaud A, Conway A, Hamze A, Ross L, Alexe G, Adane B, Nabet B, Ferguson FM, Stolte B, Wang EJ, Sun J, Darzacq X, Piccioni F, Gray NS, Fischer ES, Stegmaier K. TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma. Cancer Cell. 2021 Jul 22.
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Tang CC, Castro Andrade CD, O’Meara MJ, Yoon SH, Sato T, Brooks DJ, Bouxsein ML, Martins JDS, Wang J, Gray NS, Misof B, Roschger P, Boulin S, Klaushofer K, Velduis-Vlug A, Vegting Y, Rosen CJ, O’Connell D, Sundberg TB, Xavier RJ, Ung P, Schlessinger A, Kronenberg HM, Berdeaux R, Foretz M, Wein MN. Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption. Elife. 2021 Jun 23.
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Deng J, Thennavan A, Dolgalev I, Chen T, Li J, Marzio A, Poirier JT, Peng D, Bulatovic M, Mukhopadhyay S, Silver H, Papadopoulos E, Pyon V, Thakurdin C, Han H, Li F, Li S, Ding H, Hu H, Pan Y, Weerasekara V, Jiang B, Wang ES, Ahearn I, Philips M, Papagiannakopoulos T, Tsirigos A, Rothenberg E, Gainor J, Freeman GJ, Rudin CM, Gray NS, Hammerman PS, Pagano M, Heymach JV, Perou CM, Bardeesy N, Wong KK. ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer. Nat Cancer. 2021 May;2(5):503-514.
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Yang G, Wang J, Tan L, Munshi M, Liu X, Kofides A, Chen JG, Tsakmaklis N, Demos M, Guerrera ML, Xu L, Hunter ZR, Che J, Patterson CJ, Meid KE, Castillo J, Munshi NC, Anderson KC, Cameron M, Buhrlage S, Gray NSS, Treon SPP. The HCK/BTK inhibitor KIN-8194 is active in MYD88 driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. 2021 Jun 16.
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Arnett A, Moo KG, Flynn KJ, Sundberg TB, Johannessen L, Shamji AF, Gray NS, Decker T, Zheng Y, Gersuk VH, Rahman ZS, Levy DE, Marié IJ, Linsley PS, Xavier RJ, Khor B. The CDK8 inhibitor DCA promotes a tolerogenic chemical immunophenotype in CD4+ T cells via a novel CDK8-GATA3-FOXP3 pathway. Mol Cell Biol. 2021 Jun 14.
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Wang ES, Verano AL, Nowak RP, Yuan JC, Donovan KA, Eleuteri NA, Yue H, Ngo KH, Lizotte PH, Gokhale PC, Gray NS, Fischer ES. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.
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Vervoort SJ, Welsh SA, Devlin JR, Barbieri E, Knight DA, Offley S, Bjelosevic S, Costacurta M, Todorovski I, Kearney CJ, Sandow JJ, Fan Z, Blyth B, McLeod V, Vissers JHA, Pavic K, Martin BP, Gregory G, Demosthenous E, Zethoven M, Kong IY, Hawkins ED, Hogg SJ, Kelly MJ, Newbold A, Simpson KJ, Kauko O, Harvey KF, Ohlmeyer M, Westermarck J, Gray N, Gardini A, Johnstone RW. The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer. Cell. 2021 May 12.
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Carli ALE, Afshar-Sterle S, Rai A, Fang H, O’Keefe R, Tse J, Ferguson FM, Gray NS, Ernst M, Greening DW, Buchert M. Cancer stem cell marker DCLK1 reprograms small extracellular vesicles toward migratory phenotype in gastric cancer cells. Proteomics. 2021 May 15.
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Remenyi J, Naik RJ, Wang J, Razsolkov M, Verano A, Cai Q, Tan L, Toth R, Raggett S, Baillie C, Traynor R, Hastie CJ, Gray NS, Arthur JSC. Generation of a chemical genetic model for JAK3. Sci Rep. 2021 May 12;11(1):10093.
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Dubiella C, Pinch BJ, Koikawa K, Zaidman D, Poon E, Manz TD, Nabet B, He S, Resnick E, Rogel A, Langer EM, Daniel CJ, Seo HS, Chen Y, Adelmant G, Sharifzadeh S, Ficarro SB, Jamin Y, Martins da Costa B, Zimmerman MW, Lian X, Kibe S, Kozono S, Doctor ZM, Browne CM, Yang A, Stoler-Barak L, Shah RB, Vangos NE, Geffken EA, Oren R, Koide E, Sidi S, Shulman Z, Wang C, Marto JA, Dhe-Paganon S, Look T, Zhou XZ, Lu KP, Sears RC, Chesler L, Gray NS, London N. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021 May 10.
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Jiang B, Jiang J, Kaltheuner IH, Iniguez AB, Anand K, Ferguson FM, Ficarro SB, Seong BKA, Greifenberg AK, Dust S, Kwiatkowski NP, Marto JA, Stegmaier K, Zhang T, Geyer M, Gray NS. Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.Eur J Med Chem. 2021 Apr 20;221:113481.
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Heckler M, Ali LR, Clancy-Thompson E, Qiang L, Ventre KS, Lenehan P, Roehle K, Luoma A, Boelaars K, Peters V, McCreary J, Boschert T, Wang ES, Suo S, Marangoni F, Mempel TR, Long HW, Wucherpfennig KW, Dougan M, Gray NS, Yuan GC, Goel S, Tolaney SM, Dougan SK. Inhibition of CDK4/6 promotes CD8 T-cell memory formation. Cancer Discov. 2021 May 3.
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Du G, Jiang J, Wu Q, Henning NJ, Donovan KA, Yue H, Che J, Lu W, Fischer ES, Bardeesy N, Zhang T, Gray NS. Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. Angew Chem Int Ed Engl. 2021 Apr 29.
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Jiang B, Gao Y, Che J, Lu W, Kaltheuner IH, Dries R, Kalocsay M, Berberich MJ, Jiang J, You I, Kwiatkowski N, Riching KM, Daniels DL, Sorger PK, Geyer M, Zhang T, Gray NS. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021 Mar 22.
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Koduri V, Duplaquet L, Lampson BL, Wang AC, Sabet AH, Ishoey M, Paulk J, Teng M, Harris IS, Endress JE, Liu X, Dasilva E, Paulo JA, Briggs KJ, Doench JG, Ott CJ, Zhang T, Donovan KA, Fischer ES, Gygi SP, Gray NS, Bradner J, Medin JA, Buhrlage SJ, Oser MG, Kaelin WG Jr. Targeting oncoproteins with a positive selection assay for protein degraders. Sci Adv. 2021 Feb 5.
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Sheppard HE, Dall’Agnese A, Park WD, Shamim MH, Dubrulle J, Johnson HL, Stossi F, Cogswell P, Sommer J, Levy J, Sharifnia T, Wawer MJ, Nabet B, Gray NS, Clemons PA, Schreiber SL, Workman P, Young RA, Lin CY. Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity. Cell Rep Med. 2021 Jan 19;2(1):100188.
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Groendyke BJ, Nabet B, Mohardt ML, Zhang H, Peng K, Koide E, Coffey CR, Che J, Scott DA, Bass AJ, Gray NS. Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor. ACS Med Chem Lett. 2020 Dec 14;12(1):30-38.
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Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. Int J Mol Sci. 2021 Jan 8;22(2):E566.
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Dhimolea E, de Matos Simoes R, Kansara D, Al’Khafaji A, Bouyssou J, Weng X, Sharma S, Raja J, Awate P, Shirasaki R, Tang H, Glassner BJ, Liu Z, Gao D, Bryan J, Bender S, Roth J, Scheffer M, Jeselsohn R, Gray NS, Georgakoudi I, Vazquez F, Tsherniak A, Chen Y, Welm A, Duy C, Melnick A, Bartholdy B, Brown M, Culhane AC, Mitsiades CS. An Embryonic Diapause-like Adaptation with Suppressed Myc Activity Enables Tumor Treatment Persistence. Cancer Cell. 2021 Jan 5.
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Levine ZG, Potter SC, Joiner CM, Fei GQ, Nabet B, Sonnett M, Zachara NE, Gray NS, Paulo JA, Walker S. Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase. Proc Natl Acad Sci U S A. 2021 Jan 26.
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Shirasaki R, Matthews GM, Gandolfi S, de Matos Simoes R, Buckley DL, Raja Vora J, Sievers QL, Brüggenthies JB, Dashevsky O, Poarch H, Tang H, Bariteau MA, Sheffer M, Hu Y, Downey-Kopyscinski SL, Hengeveld PJ, Glassner BJ, Dhimolea E, Ott CJ, Zhang T, Kwiatkowski NP, Laubach JP, Schlossman RL, Richardson PG, Culhane AC, Groen RWJ, Fischer ES, Vazquez F, Tsherniak A, Hahn WC, Levy J, Auclair D, Licht JD, Keats JJ, Boise LH, Ebert BL, Bradner JE, Gray NS, Mitsiades CS. Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins.Cell Rep. 2021 Jan 5;34(1):108532.
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2020

Donovan KA, Ferguson FM, Bushman JW, Eleuteri NA, Bhunia D, Ryu S, Tan L, Shi K, Yue H, Liu X, Dobrovolsky D, Jiang B, Wang J, Hao M, You I, Teng M, Liang Y, Hatcher J, Li Z, Manz TD, Groendyke B, Hu W, Nam Y, Sengupta S, Cho H, Shin I, Agius MP, Ghobrial IM, Ma MW, Che J, Buhrlage SJ, Sim T, Gray NS, Fischer ES. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 Dec 10;183(6):1714-1731.
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Hatcher JM, Yang G, Wang L, Ficarro SB, Buhrlage S, Wu H, Marto JA, Treon SP, Gray NS. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243.
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Poon E, Liang T, Jamin Y, Walz S, Kwok C, Hakkert A, Barker K, Urban Z, Thway K, Zeid R, Hallsworth A, Box G, Ebus ME, Licciardello MP, Sbirkov Y, Lazaro G, Calton E, Costa BM, Valenti M, De Haven Brandon A, Webber H, Tardif N, Almeida GS, Christova R, Boysen G, Richards MW, Barone G, Ford A, Bayliss R, Clarke PA, De Bono J, Gray NS, Blagg J, Robinson SP, Eccles SA, Zheleva D, Bradner JE, Molenaar J, Vivanco I, Eilers M, Workman P, Lin CY, Chesler L. Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. J Clin Invest. 2020 Oct 05:134132.
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Powell CE, Du G, Che J, He Z, Donovan KA, Yue H, Wang ES, Nowak RP, Zhang T, Fischer ES, Gray NS. Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. ACS Chem Biol. 2020 Sep 28.
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Nabet B, Ferguson FM, Seong BKA, Kuljanin M, Leggett AL, Mohardt ML, Robichaud A, Conway AS, Buckley DL, Mancias JD, Bradner JE, Stegmaier K, Gray NS. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat Commun. 2020 09 18; 11(1):4687.
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Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, Kelly GP, Svejstrup JQ, Geyer M, Gray NS, Vervoort SJ, Johnstone RW. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 Apr 29.
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Jiang J, Jiang B, He Z, Ficarro SB, Che J, Marto JA, Gao Y, Zhang T, Gray NS. Discovery of Covalent MKK4/7 Dual Inhibitor. Cell Chem Biol. 2020 Sep 07.
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Weisberg E, Meng C, Case A, Sattler M, Tiv HL, Gokhale PC, Buhrlage S, Wang J, Gray N, Stone R, Liu S, Bhagwat SV, Tiu RV, Adamia S, Griffin JD. Correction: Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. 2020 Sep; 34(9):2543.
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Ferguson FM, Liu Y, Harshbarger W, Huang L, Wang J, Deng X, Capuzzi SJ, Muratov EN, Tropsha A, Muthuswamy S, Westover KD, Gray NS. Correction to “Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one Scaffold”. J Med Chem. 2020 Sep 10; 63(17):10088.
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Weisberg E, Parent A, Yang PL, Sattler M, Liu Q, Liu Q, Wang J, Meng C, Buhrlage SJ, Gray N, Griffin JD. Repurposing of Kinase Inhibitors for Treatment of COVID-19. Pharm Res. 2020 Aug 10; 37(9):167.
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Schröder M, Tan L, Wang J, Liang Y, Gray NS, Knapp S, Chaikuad A. Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities. Cell Chem Biol. 2020 Aug 04.
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Liu Y, Ferguson FM, Li L, Kuljanin M, Mills CE, Subramanian K, Harshbarger W, Gondi S, Wang J, Sorger PK, Mancias JD, Gray NS, Westover KD. Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing. Cell Chem Biol. 2020 Aug 04.
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Li Z, Powell CE, Groendyke BJ, Gero TW, Feru F, Feutrill J, Chen B, Li B, Szabo H, Gray NS, Scott DA. Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing. Bioorg Med Chem Lett. 2020 Oct 01; 30(19):127456.
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Ferguson FM, Liu Y, Harshbarger W, Huang L, Wang J, Deng X, Capuzzi SJ, Muratov EN, Tropsha A, Muthuswamy S, Westover KD, Gray NS. Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one Scaffold. J Med Chem. 2020 Jul 23; 63(14):7817-7826.
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Weisberg E, Sattler M, Yang PL, Parent A, Gray N, Griffin JD. Current therapies under investigation for COVID-19: potential COVID-19 treatments. Can J Physiol Pharmacol. 2020 Aug; 98(8):483-489.
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Liu Y, Hao M, Leggett AL, Gao Y, Ficarro SB, Che J, He Z, Olson CM, Marto JA, Kwiatkowski NP, Zhang T, Gray NS. Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. J Med Chem. 2020 Jul 09; 63(13):6708-6726.
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Klein IA, Boija A, Afeyan LK, Hawken SW, Fan M, Dall’Agnese A, Oksuz O, Henninger JE, Shrinivas K, Sabari BR, Sagi I, Clark VE, Platt JM, Kar M, McCall PM, Zamudio AV, Manteiga JC, Coffey EL, Li CH, Hannett NM, Guo YE, Decker TM, Lee TI, Zhang T, Weng JK, Taatjes DJ, Chakraborty A, Sharp PA, Chang YT, Hyman AA, Gray NS, Young RA. Partitioning of cancer therapeutics in nuclear condensates. Science. 2020 06 19; 368(6497):1386-1392.
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Giurisato E, Lonardi S, Telfer B, Lussoso S, Risa-Ebrí B, Zhang J, Russo I, Wang J, Santucci A, Finegan KG, Gray NS, Vermi W, Tournier C. Extracellular-Regulated Protein Kinase 5-Mediated Control of p21 Expression Promotes Macrophage Proliferation Associated with Tumor Growth and Metastasis. Cancer Res. 2020 Aug 15; 80(16):3319-3330.
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Fassl A, Brain C, Abu-Remaileh M, Stukan I, Butter D, Stepien P, Feit AS, Bergholz J, Michowski W, Otto T, Sheng Q, Loo A, Michael W, Tiedt R, DeAngelis C, Schiff R, Jiang B, Jovanovic B, Nowak K, Ericsson M, Cameron M, Gray N, Dillon D, Zhao JJ, Sabatini DM, Jeselsohn R, Brown M, Polyak K, Sicinski P. Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition. Sci Adv. 2020 Jun; 6(25):eabb2210.
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Jang J, To C, De Clercq DJH, Park E, Ponthier CM, Shin BH, Mushajiang M, Nowak RP, Fischer ES, Eck MJ, Jänne PA, Gray NS. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Jun 08.
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Teng M, Jiang J, He Z, Kwiatkowski NP, Donovan KA, Mills CE, Victor C, Hatcher JM, Fischer ES, Sorger PK, Zhang T, Gray NS. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020 Aug 10; 59(33):13865-13870.
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Pinch BJ, Doctor ZM, Nabet B, Browne CM, Seo HS, Mohardt ML, Kozono S, Lian X, Manz TD, Chun Y, Kibe S, Zaidman D, Daitchman D, Yeoh ZC, Vangos NE, Geffken EA, Tan L, Ficarro SB, London N, Marto JA, Buratowski S, Dhe-Paganon S, Zhou XZ, Lu KP, Gray NS. Identification of a potent and selective covalent Pin1 inhibitor. Nat Chem Biol. 2020 Sep; 16(9):979-987.
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Jaeger MG, Schwalb B, Mackowiak SD, Velychko T, Hanzl A, Imrichova H, Brand M, Agerer B, Chorn S, Nabet B, Ferguson FM, Müller AC, Bergthaler A, Gray NS, Bradner JE, Bock C, Hnisz D, Cramer P, Winter GE. Selective Mediator dependence of cell-type-specifying transcription. Nat Genet. 2020 07; 52(7):719-727.
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Hsu A, Duan Q, McMahon S, Huang Y, Wood SA, Gray NS, Wang B, Bruneau BG, Haldar SM. Salt-inducible kinase 1 maintains HDAC7 stability to promote pathologic cardiac remodeling. J Clin Invest. 2020 Jun 01; 130(6):2966-2977.
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Gurbani D, Du G, Henning NJ, Rao S, Bera AK, Zhang T, Gray NS, Westover KD. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020; 7:81.
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Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, Kelly GP, Svejstrup JQ, Geyer M, Gray NS, Vervoort SJ, Johnstone RW. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 May; 6(18).
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Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, Kelly GP, Svejstrup JQ, Geyer M, Gray NS, Vervoort SJ, Johnstone RW. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 May; 6(18):eaaz5041.
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Gasic I, Groendyke BJ, Nowak RP, Yuan JC, Kalabathula J, Fischer ES, Gray NS, Mitchison TJ. Tubulin Resists Degradation by Cereblon-Recruiting PROTACs. Cells. 2020 Apr 27; 9(5).
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Manz TD, Sivakumaren SC, Ferguson FM, Zhang T, Yasgar A, Seo HS, Ficarro SB, Card JD, Shim H, Miduturu CV, Simeonov A, Shen M, Marto JA, Dhe-Paganon S, Hall MD, Cantley LC, Gray NS. Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. J Med Chem. 2020 05 14; 63(9):4880-4895.
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Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell. 2020 Apr 30; 181(3):702-715.e20.
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Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J, Ng RWS, Sulahian R, Li L, Poulin EJ, Huang L, Koren J, Dieguez-Martinez N, Espinosa S, Zeng Z, Corona CR, Vasta JD, Ohi R, Sim T, Kim ND, Harshbarger W, Lizcano JM, Robers MB, Muthaswamy S, Lin CY, Look AT, Haigis KM, Mancias JD, Wolpin BM, Aguirre AJ, Hahn WC, Westover KD, Gray NS. Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 06; 16(6):635-643.
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Teng M, Ficarro SB, Yoon H, Che J, Zhou J, Fischer ES, Marto JA, Zhang T, Gray NS. Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface. ACS Med Chem Lett. 2020 Jun 11; 11(6):1269-1273.
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Santana-Codina N, Chandhoke AS, Yu Q, Malachowska B, Kuljanin M, Gikandi A, Stanczak M, Gableske S, Jedrychowski MP, Scott DA, Aguirre AJ, Fendler W, Gray NS, Mancias JD. Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics. Cell Rep. 2020 Mar 31; 30(13):4584-4599.e4.
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Ogino A, Choi J, Lin M, Wilkens MK, Calles A, Xu M, Adeni AE, Chambers ES, Capelletti M, Butaney M, Gray NS, Gokhale PC, Palakurthi S, Kirschmeier P, Oxnard GR, Sholl LM, Jänne PA. Genomic and pathological heterogeneity in clinically diagnosed small cell lung cancer in never/light smokers identifies therapeutically targetable alterations. Mol Oncol. 2020 Mar 19.
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Lochhead PA, Tucker JA, Tatum NJ, Wang J, Oxley D, Kidger AM, Johnson VP, Cassidy MA, Gray NS, Noble MEM, Cook SJ. Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors. Nat Commun. 2020 03 13; 11(1):1383.
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Sivakumaren SC, Shim H, Zhang T, Ferguson FM, Lundquist MR, Browne CM, Seo HS, Paddock MN, Manz TD, Jiang B, Hao MF, Krishnan P, Wang DG, Yang TJ, Kwiatkowski NP, Ficarro SB, Cunningham JM, Marto JA, Dhe-Paganon S, Cantley LC, Gray NS. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 2020 May 21; 27(5):525-537.e6.
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Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. Correction: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2020 Feb 28; 295(9):2886.
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Xiao H, Jedrychowski MP, Schweppe DK, Huttlin EL, Yu Q, Heppner DE, Li J, Long J, Mills EL, Szpyt J, He Z, Du G, Garrity R, Reddy A, Vaites LP, Paulo JA, Zhang T, Gray NS, Gygi SP, Chouchani ET. A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging. Cell. 2020 03 05; 180(5):968-983.e24.
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Liu J, Chen H, Ma L, He Z, Wang D, Liu Y, Lin Q, Zhang T, Gray N, Kaniskan HÜ, Jin J, Wei W. Light-induced control of protein destruction by opto-PROTAC. Sci Adv. 2020 02; 6(8):eaay5154.
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Yang J, Meng C, Weisberg E, Case A, Lamberto I, Magin RS, Adamia S, Wang J, Gray N, Liu S, Stone R, Sattler M, Buhrlage S, Griffin JD. Inhibition of the deubiquitinase USP10 induces degradation of SYK. Br J Cancer. 2020 Apr; 122(8):1175-1184.
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Munshi M, Liu X, Chen JG, Xu L, Tsakmaklis N, Demos MG, Kofides A, Guerrera ML, Jimenez C, Chan GG, Hunter ZR, Palomba ML, Argyropoulos KV, Meid K, Keezer A, Gustine J, Dubeau T, Castillo JJ, Patterson CJ, Wang J, Buhrlage SJ, Gray NS, Treon SP, Yang G. SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas. Blood Cancer J. 2020 01 31; 10(1):12.
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Du G, Rao S, Gurbani D, Henning NJ, Jiang J, Che J, Yang A, Ficarro SB, Marto JA, Aguirre AJ, Sorger PK, Westover KD, Zhang T, Gray NS. Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine. J Med Chem. 2020 02 27; 63(4):1624-1641.
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Weisberg E, Meng C, Case AE, Tiv HL, Gokhale PC, Buhrlage SJ, Yang J, Liu X, Wang J, Gray N, Adamia S, Sattler M, Stone R, Griffin JD. Effects of the multi-kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia. J Cell Mol Med. 2020 Mar; 24(5):2968-2980.
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Weisberg E, Meng C, Case AE, Tiv HL, Gokhale PC, Toure AA, Buhrlage S, Liu X, Wang J, Gray N, Stone R, Adamia S, Winer E, Sattler M, Griffin JD. The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations. J Cell Mol Med. 2020 Feb; 24(3):2145-2156.
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Kurppa KJ, Liu Y, To C, Zhang T, Fan M, Vajdi A, Knelson EH, Xie Y, Lim K, Cejas P, Portell A, Lizotte PH, Ficarro SB, Li S, Chen T, Haikala HM, Wang H, Bahcall M, Gao Y, Shalhout S, Boettcher S, Shin BH, Thai T, Wilkens MK, Tillgren ML, Mushajiang M, Xu M, Choi J, Bertram AA, Ebert BL, Beroukhim R, Bandopadhayay P, Awad MM, Gokhale PC, Kirschmeier PT, Marto JA, Camargo FD, Haq R, Paweletz CP, Wong KK, Barbie DA, Long HW, Gray NS, Jänne PA. Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. Cancer Cell. 2020 01 13; 37(1):104-122.e12.
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Kim JW, Berrios C, Kim M, Schade AE, Adelmant G, Yeerna H, Damato E, Iniguez AB, Florens L, Washburn MP, Stegmaier K, Gray NS, Tamayo P, Gjoerup O, Marto JA, DeCaprio J, Hahn WC. STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells. Elife. 2020 Jan 08; 9.
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Groendyke BJ, Powell CE, Feru F, Gero TW, Li Z, Szabo H, Pang K, Feutrill J, Chen B, Li B, Gray NS, Scott DA. Benzopyrimidodiazepinone inhibitors of TNK2. Bioorg Med Chem Lett. 2020 02 15; 30(4):126948.
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Tarumoto Y, Lin S, Wang J, Milazzo JP, Xu Y, Lu B, Yang Z, Wei Y, Polyanskaya S, Wunderlich M, Gray NS, Stegmaier K, Vakoc CR. Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo. Blood. 2020 01 02; 135(1):56-70.
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de Wispelaere M, Carocci M, Burri DJ, Neidermyer WJ, Olson CM, Roggenbach I, Liang Y, Wang J, Whelan SPJ, Gray NS, Yang PL. A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation. J Biol Chem. 2020 02 07; 295(6):1694-1703.
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Zeng M, Xiong Y, Safaee N, Nowak RP, Donovan KA, Yuan CJ, Nabet B, Gero TW, Feru F, Li L, Gondi S, Ombelets LJ, Quan C, Jänne PA, Kostic M, Scott DA, Westover KD, Fischer ES, Gray NS. Exploring Targeted Degradation Strategy for Oncogenic KRASG12C. Cell Chem Biol. 2020 01 16; 27(1):19-31.e6.
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Zhang H, Christensen CL, Dries R, Oser MG, Deng J, Diskin B, Li F, Pan Y, Zhang X, Yin Y, Papadopoulos E, Pyon V, Thakurdin C, Kwiatkowski N, Jani K, Rabin AR, Castro DM, Chen T, Silver H, Huang Q, Bulatovic M, Dowling CM, Sundberg B, Leggett A, Ranieri M, Han H, Li S, Yang A, Labbe KE, Almonte C, Sviderskiy VO, Quinn M, Donaghue J, Wang ES, Zhang T, He Z, Velcheti V, Hammerman PS, Freeman GJ, Bonneau R, Kaelin WG, Sutherland KD, Kersbergen A, Aguirre AJ, Yuan GC, Rothenberg E, Miller G, Gray NS, Wong KK. CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer. Cancer Cell. 2020 01 13; 37(1):37-54.e9.
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You I, Erickson EC, Donovan KA, Eleuteri NA, Fischer ES, Gray NS, Toker A. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 01 16; 27(1):66-73.e7.
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Chopra SS, Jenney A, Palmer A, Niepel M, Chung M, Mills C, Sivakumaren SC, Liu Q, Chen JY, Yapp C, Asara JM, Gray NS, Sorger PK. Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. Cell Syst. 2020 01 22; 10(1):66-81.e11.
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Li Z, Pinch BJ, Olson CM, Donovan KA, Nowak RP, Mills CE, Scott DA, Doctor ZM, Eleuteri NA, Chung M, Sorger PK, Fischer ES, Gray NS. Development and Characterization of a Wee1 Kinase Degrader. Cell Chem Biol. 2020 01 16; 27(1):57-65.e9.
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Faust TB, Yoon H, Nowak RP, Donovan KA, Li Z, Cai Q, Eleuteri NA, Zhang T, Gray NS, Fischer ES. Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol. 2020 01; 16(1):7-14.
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Manz TD, Sivakumaren SC, Yasgar A, Hall MD, Davis MI, Seo HS, Card JD, Ficarro SB, Shim H, Marto JA, Dhe-Paganon S, Sasaki AT, Boxer MB, Simeonov A, Cantley LC, Shen M, Zhang T, Ferguson FM, Gray NS. Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. ACS Med Chem Lett. 2020 Mar 12; 11(3):346-352.
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2019

Lian W, Jang J, Potisopon S, Li PC, Rahmeh A, Wang J, Kwiatkowski NP, Gray NS, Yang PL. Correction to Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. ACS Infect Dis. 2019 Dec 13; 5(12):2176.
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De Clercq DJH, Heppner DE, To C, Jang J, Park E, Yun CH, Mushajiang M, Shin BH, Gero TW, Scott DA, Jänne PA, Eck MJ, Gray NS. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. ACS Med Chem Lett. 2019 Nov 14; 10(11):1549-1553.
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Menzl I, Zhang T, Berger-Becvar A, Grausenburger R, Heller G, Prchal-Murphy M, Edlinger L, Knab VM, Uras IZ, Grundschober E, Bauer K, Roth M, Skucha A, Liu Y, Hatcher JM, Liang Y, Kwiatkowski NP, Fux D, Hoelbl-Kovacic A, Kubicek S, Melo JV, Valent P, Weichhart T, Grebien F, Zuber J, Gray NS, Sexl V. A kinase-independent role for CDK8 in BCR-ABL1+ leukemia. Nat Commun. 2019 10 18; 10(1):4741.
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Zhang T, Hatcher JM, Teng M, Gray NS, Kostic M. Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. Cell Chem Biol. 2019 11 21; 26(11):1486-1500.
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Sulahian R, Kwon JJ, Walsh KH, Pailler E, Bosse TL, Thaker M, Almanza D, Dempster JM, Pan J, Piccioni F, Dumont N, Gonzalez A, Rennhack J, Nabet B, Bachman JA, Goodale A, Lee Y, Bagul M, Liao R, Navarro A, Yuan TL, Ng RWS, Raghavan S, Gray NS, Tsherniak A, Vazquez F, Root DE, Firestone AJ, Settleman J, Hahn WC, Aguirre AJ. Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. Cell Rep. 2019 10 01; 29(1):118-134.e8.
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Remillard D, Buckley DL, Seo HS, Ferguson FM, Dhe-Paganon S, Bradner JE, Gray NS. Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med Chem Lett. 2019 Oct 10; 10(10):1443-1449.
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Weisberg E, Meng C, Case A, Sattler M, Tiv HL, Gokhale PC, Buhrlage S, Wang J, Gray N, Stone R, Liu S, Bhagwat SV, Tiu RV, Adamia S, Griffin JD. Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. 2020 02; 34(2):625-629.
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Debruyne DN, Dries R, Sengupta S, Seruggia D, Gao Y, Sharma B, Huang H, Moreau L, McLane M, Day DS, Marco E, Chen T, Gray NS, Wong KK, Orkin SH, Yuan GC, Young RA, George RE. BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells. Nature. 2019 08; 572(7771):676-680.
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de Wispelaere M, Du G, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nat Commun. 2019 08 01; 10(1):3468.
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Tang X, Drotar J, Li K, Clairmont CD, Brumm AS, Sullins AJ, Wu H, Liu XS, Wang J, Gray NS, Sur M, Jaenisch R. Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice. Sci Transl Med. 2019 07 31; 11(503).
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Weisberg E, Meng C, Case AE, Sattler M, Tiv HL, Gokhale PC, Buhrlage SJ, Liu X, Yang J, Wang J, Gray N, Stone RM, Adamia S, Dubreuil P, Letard S, Griffin JD. Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies. Br J Haematol. 2019 11; 187(4):488-501.
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Ferguson FM, Doctor ZM, Ficarro SB, Marto JA, Kim ND, Sim T, Gray NS. Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Bioorg Med Chem Lett. 2019 08 01; 29(15):1985-1993.
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Scott DA, Hatcher JM, Liu H, Fu M, Du G, Fontán L, Us I, Casalena G, Qiao Q, Wu H, Melnick A, Gray NS. Quinoline and thiazolopyridine allosteric inhibitors of MALT1. Bioorg Med Chem Lett. 2019 07 15; 29(14):1694-1698.
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Rodon Ahnert J, Gray N, Mok T, Gainor J. What It Takes to Improve a First-Generation Inhibitor to a Second- or Third-Generation Small Molecule. Am Soc Clin Oncol Educ Book. 2019 Jan; 39:196-205.
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Du L, Anderson A, Nguyen K, Ojeda SS, Ortiz-Rivera I, Nguyen TN, Zhang T, Kaoud TS, Gray NS, Dalby KN, Tsai KY. JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells. ACS Chem Biol. 2019 07 19; 14(7):1426-1435.
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To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, Eck MJ, Gray NS, Jänne PA. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 07; 9(7):926-943.
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Zhao X, Ren Y, Lawlor M, Shah BD, Park PMC, Lwin T, Wang X, Liu K, Wang M, Gao J, Li T, Xu M, Silva AS, Lee K, Zhang T, Koomen JM, Jiang H, Sudalagunta PR, Meads MB, Cheng F, Bi C, Fu K, Fan H, Dalton WS, Moscinski LC, Shain KH, Sotomayor EM, Wang GG, Gray NS, Cleveland JL, Qi J, Tao J. BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models. Cancer Cell. 2019 05 13; 35(5):752-766.e9.
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Krajewska M, Dries R, Grassetti AV, Dust S, Gao Y, Huang H, Sharma B, Day DS, Kwiatkowski N, Pomaville M, Dodd O, Chipumuro E, Zhang T, Greenleaf AL, Yuan GC, Gray NS, Young RA, Geyer M, Gerber SA, George RE. CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation. Nat Commun. 2019 04 15; 10(1):1757.
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Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Tan L, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, Westover KD, Sorger PK, Gray NS. Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chem Biol. 2019 06 20; 26(6):818-829.e9.
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Moret N, Clark NA, Hafner M, Wang Y, Lounkine E, Medvedovic M, Wang J, Gray N, Jenkins J, Sorger PK. Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries. Cell Chem Biol. 2019 05 16; 26(5):765-777.e3.
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Hatcher JM, Du G, Fontán L, Us I, Qiao Q, Chennamadhavuni S, Shao J, Wu H, Melnick A, Gray NS, Scott DA. Peptide-based covalent inhibitors of MALT1 paracaspase. Bioorg Med Chem Lett. 2019 06 01; 29(11):1336-1339.
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Jiang B, Wang ES, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 05 06; 58(19):6321-6326.
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Ferguson FM, Doctor ZM, Ficarro SB, Browne CM, Marto JA, Johnson JL, Yaron TM, Cantley LC, Kim ND, Sim T, Berberich MJ, Kalocsay M, Sorger PK, Gray NS. Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity. Cell Chem Biol. 2019 06 20; 26(6):804-817.e12.
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Silva MC, Ferguson FM, Cai Q, Donovan KA, Nandi G, Patnaik D, Zhang T, Huang HT, Lucente DE, Dickerson BC, Mitchison TJ, Fischer ES, Gray NS, Haggarty SJ. Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. Elife. 2019 03 25; 8.
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Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 06 20; 26(6):792-803.e10.
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Hsieh HHS, Agarwal S, Cholok DJ, Loder SJ, Kaneko K, Huber A, Chung MT, Ranganathan K, Habbouche J, Li J, Butts J, Reimer J, Kaura A, Drake J, Breuler C, Priest CR, Nguyen J, Brownley C, Peterson J, Ozgurel SU, Niknafs YS, Li S, Inagaki M, Scott G, Krebsbach PH, Longaker MT, Westover K, Gray N, Ninomiya-Tsuji J, Mishina Y, Levi B. Coordinating Tissue Regeneration Through Transforming Growth Factor-ß Activated Kinase 1 Inactivation and Reactivation. Stem Cells. 2019 06; 37(6):766-778.
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Rao S, Du G, Hafner M, Subramanian K, Sorger PK, Gray NS. A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers. J Biol Chem. 2019 05 24; 294(21):8664-8673.
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Pitts J, Hsia CY, Lian W, Wang J, Pfeil MP, Kwiatkowski N, Li Z, Jang J, Gray NS, Yang PL. Identification of small molecule inhibitors targeting the Zika virus envelope protein. Antiviral Res. 2019 04; 164:147-153.
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Wang L, Ferrao R, Li Q, Hatcher JM, Choi HG, Buhrlage SJ, Gray NS, Wu H. Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4). J Biol Chem. 2019 03 22; 294(12):4511-4519.
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Sharifnia T, Wawer MJ, Chen T, Huang QY, Weir BA, Sizemore A, Lawlor MA, Goodale A, Cowley GS, Vazquez F, Ott CJ, Francis JM, Sassi S, Cogswell P, Sheppard HE, Zhang T, Gray NS, Clarke PA, Blagg J, Workman P, Sommer J, Hornicek F, Root DE, Hahn WC, Bradner JE, Wong KK, Clemons PA, Lin CY, Kotz JD, Schreiber SL. Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nat Med. 2019 02; 25(2):292-300.
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Li PC, Jang J, Hsia CY, Groomes PV, Lian W, de Wispelaere M, Pitts JD, Wang J, Kwiatkowski N, Gray NS, Yang PL. Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo. ACS Infect Dis. 2019 03 08; 5(3):460-472.
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Brand M, Jiang B, Bauer S, Donovan KA, Liang Y, Wang ES, Nowak RP, Yuan JC, Zhang T, Kwiatkowski N, Müller AC, Fischer ES, Gray NS, Winter GE. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol. 2019 02 21; 26(2):300-306.e9.
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Browne CM, Jiang B, Ficarro SB, Doctor ZM, Johnson JL, Card JD, Sivakumaren SC, Alexander WM, Yaron TM, Murphy CJ, Kwiatkowski NP, Zhang T, Cantley LC, Gray NS, Marto JA. A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 01 09; 141(1):191-203.
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Dobrovolsky D, Wang ES, Morrow S, Leahy C, Faust T, Nowak RP, Donovan KA, Yang G, Li Z, Fischer ES, Treon SP, Weinstock DM, Gray NS. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood. 2019 02 28; 133(9):952-961.
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2018

Brien GL, Remillard D, Shi J, Hemming ML, Chabon J, Wynne K, Dillon ET, Cagney G, Van Mierlo G, Baltissen MP, Vermeulen M, Qi J, Fröhling S, Gray NS, Bradner JE, Vakoc CR, Armstrong SA. Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife. 2018 11 15; 7.
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Zeng M, Kwiatkowski NP, Zhang T, Nabet B, Xu M, Liang Y, Quan C, Wang J, Hao M, Palakurthi S, Zhou S, Zeng Q, Kirschmeier PT, Meghani K, Leggett AL, Qi J, Shapiro GI, Liu JF, Matulonis UA, Lin CY, Konstantinopoulos PA, Gray NS. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 11 13; 7.
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Michel BC, D’Avino AR, Cassel SH, Mashtalir N, McKenzie ZM, McBride MJ, Valencia AM, Zhou Q, Bocker M, Soares LMM, Pan J, Remillard DI, Lareau CA, Zullow HJ, Fortoul N, Gray NS, Bradner JE, Chan HM, Kadoch C. A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation. Nat Cell Biol. 2018 12; 20(12):1410-1420.
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Lizotte PH, Hong RL, Luster TA, Cavanaugh ME, Taus LJ, Wang S, Dhaneshwar A, Mayman N, Yang A, Kulkarni M, Badalucco L, Fitzpatrick E, Kao HF, Kuraguchi M, Bittinger M, Kirschmeier PT, Gray NS, Barbie DA, Jänne PA. A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing. Cancer Immunol Res. 2018 12; 6(12):1511-1523.
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Tusa I, Cheloni G, Poteti M, Gozzini A, DeSouza NH, Shan Y, Deng X, Gray NS, Li S, Rovida E, Dello Sbarba P. Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells. Stem Cell Reports. 2018 10 09; 11(4):929-943.
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Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T. First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia. J Med Chem. 2018 09 27; 61(18):8353-8373.
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Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martínez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS. Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains. ACS Chem Biol. 2018 09 21; 13(9):2438-2448.
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Lian W, Jang J, Potisopon S, Li PC, Rahmeh A, Wang J, Kwiatkowski NP, Gray NS, Yang PL. Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. ACS Infect Dis. 2018 09 14; 4(9):1395-1406.
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Czarna A, Wang J, Zelencova D, Liu Y, Deng X, Choi HG, Zhang T, Zhou W, Chang JW, Kildalsen H, Seternes OM, Gray NS, Engh RA, Rothweiler U. Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. J Med Chem. 2018 09 13; 61(17):7560-7572.
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Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS. Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor. Angew Chem Int Ed Engl. 2018 09 03; 57(36):11629-11633.
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Fontán L, Qiao Q, Hatcher JM, Casalena G, Us I, Teater M, Durant M, Du G, Xia M, Bilchuk N, Chennamadhavuni S, Palladino G, Inghirami G, Philippar U, Wu H, Scott DA, Gray NS, Melnick A. Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth. J Clin Invest. 2018 10 01; 128(10):4397-4412.
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Chen S, Cai C, Sowalsky AG, Ye H, Ma F, Yuan X, Simon NI, Gray NS, Balk SP. BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer. Cancer Res. 2018 09 15; 78(18):5203-5215.
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Zhou W, Whiteley AT, de Oliveira Mann CC, Morehouse BR, Nowak RP, Fischer ES, Gray NS, Mekalanos JJ, Kranzusch PJ. Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell. 2018 07 12; 174(2):300-311.e11.
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Chao LH, Jang J, Johnson A, Nguyen A, Gray NS, Yang PL, Harrison SC. How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion. Elife. 2018 07 12; 7.
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Tusa I, Cheloni G, Poteti M, Gozzini A, Deng X, Gray NS, Li S, Dello Sbarba P, Rovida E. Targeting chronic myeloid leukemia stem cells with ERK5 pathway inhibitors. J Biol Regul Homeost Agents. 2018 Jul-Aug; 32(4 Suppl. 1):36.
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de Wispelaere M, Lian W, Potisopon S, Li PC, Jang J, Ficarro SB, Clark MJ, Zhu X, Kaplan JB, Pitts JD, Wales TE, Wang J, Engen JR, Marto JA, Gray NS, Yang PL. Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein. Cell Chem Biol. 2018 08 16; 25(8):1006-1016.e8.
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Nowak RP, DeAngelo SL, Buckley D, He Z, Donovan KA, An J, Safaee N, Jedrychowski MP, Ponthier CM, Ishoey M, Zhang T, Mancias JD, Gray NS, Bradner JE, Fischer ES. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 07; 14(7):706-714.
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Weir MC, Shu ST, Patel RK, Hellwig S, Chen L, Tan L, Gray NS, Smithgall TE. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 06 15; 13(6):1551-1559.
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Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Jänne PA, George RE, Gray NS. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2018 05 10; 61(9):4249-4255.
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Bockorny B, Rusan M, Chen W, Liao RG, Li Y, Piccioni F, Wang J, Tan L, Thorner AR, Li T, Zhang Y, Miao C, Ovesen T, Shapiro GI, Kwiatkowski DJ, Gray NS, Meyerson M, Hammerman PS, Bass AJ. RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade. . 2018 07; 17(7):1526-1539.
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Nabet B, Gray NS. It Takes Two To Target: A Study in KRAS Dimerization. Biochemistry. 2018 04 24; 57(16):2289-2290.
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Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, Wong KK, Gray NS, Bradner JE. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018 05; 14(5):431-441.
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Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Jun 14; 9(6):540-545.
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Ferguson FM, Gray NS. Kinase inhibitors: the road ahead. Nat Rev Drug Discov. 2018 05; 17(5):353-377.
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Wang Y, Li YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ. Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 2018 03 12; 7.
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Giurisato E, Xu Q, Lonardi S, Telfer B, Russo I, Pearson A, Finegan KG, Wang W, Wang J, Gray NS, Vermi W, Xia Z, Tournier C. Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition. Proc Natl Acad Sci U S A. 2018 03 20; 115(12):E2801-E2810.
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Gechijian LN, Buckley DL, Lawlor MA, Reyes JM, Paulk J, Ott CJ, Winter GE, Erb MA, Scott TG, Xu M, Seo HS, Dhe-Paganon S, Kwiatkowski NP, Perry JA, Qi J, Gray NS, Bradner JE. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 04; 14(4):405-412.
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Chen JG, Liu X, Munshi M, Xu L, Tsakmaklis N, Demos MG, Kofides A, Guerrera ML, Chan GG, Patterson CJ, Meid K, Gustine J, Dubeau T, Severns P, Castillo JJ, Hunter ZR, Wang J, Buhrlage SJ, Gray NS, Treon SP, Yang G. BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism. Blood. 2018 05 03; 131(18):2047-2059.
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Tusa I, Gagliardi S, Tubita A, Pandolfi S, Urso C, Borgognoni L, Wang J, Deng X, Gray NS, Stecca B, Rovida E. ERK5 is activated by oncogenic BRAF and promotes melanoma growth. Oncogene. 2018 05; 37(19):2601-2614.
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Hatcher JM, Wu G, Zeng C, Zhu J, Meng F, Patel S, Wang W, Ficarro SB, Leggett AL, Powell CE, Marto JA, Zhang K, Ki Ngo JC, Fu XD, Zhang T, Gray NS. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 04 19; 25(4):460-470.e6.
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Jeselsohn R, Bergholz JS, Pun M, Cornwell M, Liu W, Nardone A, Xiao T, Li W, Qiu X, Buchwalter G, Feiglin A, Abell-Hart K, Fei T, Rao P, Long H, Kwiatkowski N, Zhang T, Gray N, Melchers D, Houtman R, Liu XS, Cohen O, Wagle N, Winer EP, Zhao J, Brown M. Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations. Cancer Cell. 2018 02 12; 33(2):173-186.e5.
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Eliades P, Abraham BJ, Ji Z, Miller DM, Christensen CL, Kwiatkowski N, Kumar R, Njauw CN, Taylor M, Miao B, Zhang T, Wong KK, Gray NS, Young RA, Tsao H. High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma. J Invest Dermatol. 2018 07; 138(7):1582-1590.
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Zheng Y, Sethi R, Mangala LS, Taylor C, Goldsmith J, Wang M, Masuda K, Karaminejadranjbar M, Mannion D, Miranda F, Herrero-Gonzalez S, Hellner K, Chen F, Alsaadi A, Albukhari A, Fotso DC, Yau C, Jiang D, Pradeep S, Rodriguez-Aguayo C, Lopez-Berestein G, Knapp S, Gray NS, Campo L, Myers KA, Dhar S, Ferguson D, Bast RC, Sood AK, von Delft F, Ahmed AA. Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation. Nat Commun. 2018 02 02; 9(1):476.
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Iniguez AB, Stolte B, Wang EJ, Conway AS, Alexe G, Dharia NV, Kwiatkowski N, Zhang T, Abraham BJ, Mora J, Kalev P, Leggett A, Chowdhury D, Benes CH, Young RA, Gray NS, Stegmaier K. EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma. Cancer Cell. 2018 02 12; 33(2):202-216.e6.
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Gao Y, Zhang T, Terai H, Ficarro SB, Kwiatkowski N, Hao MF, Sharma B, Christensen CL, Chipumuro E, Wong KK, Marto JA, Hammerman PS, Gray NS, George RE. Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chem Biol. 2018 02 15; 25(2):135-142.e5.
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Terai H, Kitajima S, Potter DS, Matsui Y, Quiceno LG, Chen T, Kim TJ, Rusan M, Thai TC, Piccioni F, Donovan KA, Kwiatkowski N, Hinohara K, Wei G, Gray NS, Fischer ES, Wong KK, Shimamura T, Letai A, Hammerman PS, Barbie DA. ER Stress Signaling Promotes the Survival of Cancer “Persister Cells” Tolerant to EGFR Tyrosine Kinase Inhibitors. Cancer Res. 2018 02 15; 78(4):1044-1057.
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Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL, Haas W, Nomanbhoy T, Fischer ES, Young RA, Bradner JE, Winter GE, Gray NS. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat Chem Biol. 2018 02; 14(2):163-170.
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2017

Weintraub AS, Li CH, Zamudio AV, Sigova AA, Hannett NM, Day DS, Abraham BJ, Cohen MA, Nabet B, Buckley DL, Guo YE, Hnisz D, Jaenisch R, Bradner JE, Gray NS, Young RA. YY1 Is a Structural Regulator of Enhancer-Promoter Loops. Cell. 2017 Dec 14; 171(7):1573-1588.e28.
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Wang L, Qiao Q, Ferrao R, Shen C, Hatcher JM, Buhrlage SJ, Gray NS, Wu H. Crystal structure of human IRAK1. Proc Natl Acad Sci U S A. 2017 12 19; 114(51):13507-13512.
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Subramanian A, Narayan R, Corsello SM, Peck DD, Natoli TE, Lu X, Gould J, Davis JF, Tubelli AA, Asiedu JK, Lahr DL, Hirschman JE, Liu Z, Donahue M, Julian B, Khan M, Wadden D, Smith IC, Lam D, Liberzon A, Toder C, Bagul M, Orzechowski M, Enache OM, Piccioni F, Johnson SA, Lyons NJ, Berger AH, Shamji AF, Brooks AN, Vrcic A, Flynn C, Rosains J, Takeda DY, Hu R, Davison D, Lamb J, Ardlie K, Hogstrom L, Greenside P, Gray NS, Clemons PA, Silver S, Wu X, Zhao WN, Read-Button W, Wu X, Haggarty SJ, Ronco LV, Boehm JS, Schreiber SL, Doench JG, Bittker JA, Root DE, Wong B, Golub TR. A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles. Cell. 2017 Nov 30; 171(6):1437-1452.e17.
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Keenan AB, Jenkins SL, Jagodnik KM, Koplev S, He E, Torre D, Wang Z, Dohlman AB, Silverstein MC, Lachmann A, Kuleshov MV, Ma’ayan A, Stathias V, Terryn R, Cooper D, Forlin M, Koleti A, Vidovic D, Chung C, Schürer SC, Vasiliauskas J, Pilarczyk M, Shamsaei B, Fazel M, Ren Y, Niu W, Clark NA, White S, Mahi N, Zhang L, Kouril M, Reichard JF, Sivaganesan S, Medvedovic M, Meller J, Koch RJ, Birtwistle MR, Iyengar R, Sobie EA, Azeloglu EU, Kaye J, Osterloh J, Haston K, Kalra J, Finkbiener S, Li J, Milani P, Adam M, Escalante-Chong R, Sachs K, Lenail A, Ramamoorthy D, Fraenkel E, Daigle G, Hussain U, Coye A, Rothstein J, Sareen D, Ornelas L, Banuelos M, Mandefro B, Ho R, Svendsen CN, Lim RG, Stocksdale J, Casale MS, Thompson TG, Wu J, Thompson LM, Dardov V, Venkatraman V, Matlock A, Van Eyk JE, Jaffe JD, Papanastasiou M, Subramanian A, Golub TR, Erickson SD, Fallahi-Sichani M, Hafner M, Gray NS, Lin JR, Mills CE, Muhlich JL, Niepel M, Shamu CE, Williams EH, Wrobel D, Sorger PK, Heiser LM, Gray JW, Korkola JE, Mills GB, LaBarge M, Feiler HS, Dane MA, Bucher E, Nederlof M, Sudar D, Gross S, Kilburn DF, Smith R, Devlin K, Margolis R, Derr L, Lee A, Pillai A. The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations. Cell Syst. 2018 01 24; 6(1):13-24.
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Huang HT, Dobrovolsky D, Paulk J, Yang G, Weisberg EL, Doctor ZM, Buckley DL, Cho JH, Ko E, Jang J, Shi K, Choi HG, Griffin JD, Li Y, Treon SP, Fischer ES, Bradner JE, Tan L, Gray NS. A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chem Biol. 2018 01 18; 25(1):88-99.e6.
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Deng J, Wang ES, Jenkins RW, Li S, Dries R, Yates K, Chhabra S, Huang W, Liu H, Aref AR, Ivanova E, Paweletz CP, Bowden M, Zhou CW, Herter-Sprie GS, Sorrentino JA, Bisi JE, Lizotte PH, Merlino AA, Quinn MM, Bufe LE, Yang A, Zhang Y, Zhang H, Gao P, Chen T, Cavanaugh ME, Rode AJ, Haines E, Roberts PJ, Strum JC, Richards WG, Lorch JH, Parangi S, Gunda V, Boland GM, Bueno R, Palakurthi S, Freeman GJ, Ritz J, Haining WN, Sharpless NE, Arthanari H, Shapiro GI, Barbie DA, Gray NS, Wong KK. CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation. Cancer Discov. 2018 02; 8(2):216-233.
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Rusan M, Li K, Li Y, Christensen CL, Abraham BJ, Kwiatkowski N, Buczkowski KA, Bockorny B, Chen T, Li S, Rhee K, Zhang H, Chen W, Terai H, Tavares T, Leggett AL, Li T, Wang Y, Zhang T, Kim TJ, Hong SH, Poudel-Neupane N, Silkes M, Mudianto T, Tan L, Shimamura T, Meyerson M, Bass AJ, Watanabe H, Gray NS, Young RA, Wong KK, Hammerman PS. Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression. Cancer Discov. 2018 01; 8(1):59-73.
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Kalan S, Amat R, Schachter MM, Kwiatkowski N, Abraham BJ, Liang Y, Zhang T, Olson CM, Larochelle S, Young RA, Gray NS, Fisher RP. Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors. Cell Rep. 2017 Oct 10; 21(2):467-481.
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Wong RWJ, Ngoc PCT, Leong WZ, Yam AWY, Zhang T, Asamitsu K, Iida S, Okamoto T, Ueda R, Gray NS, Ishida T, Sanda T. Enhancer profiling identifies critical cancer genes and characterizes cell identity in adult T-cell leukemia. Blood. 2017 11 23; 130(21):2326-2338.
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Weisberg EL, Schauer NJ, Yang J, Lamberto I, Doherty L, Bhatt S, Nonami A, Meng C, Letai A, Wright R, Tiv H, Gokhale PC, Ritorto MS, De Cesare V, Trost M, Christodoulou A, Christie A, Weinstock DM, Adamia S, Stone R, Chauhan D, Anderson KC, Seo HS, Dhe-Paganon S, Sattler M, Gray NS, Griffin JD, Buhrlage SJ. Inhibition of USP10 induces degradation of oncogenic FLT3. Nat Chem Biol. 2017 Dec; 13(12):1207-1215.
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Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 2017 09 19; 6.
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Gilbert AS, Seoane PI, Sephton-Clark P, Bojarczuk A, Hotham R, Giurisato E, Sarhan AR, Hillen A, Velde GV, Gray NS, Alessi DR, Cunningham DL, Tournier C, Johnston SA, May RC. Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5. Sci Adv. 2017 08; 3(8):e1700898.
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Johannessen L, Sundberg TB, O’Connell DJ, Kolde R, Berstler J, Billings KJ, Khor B, Seashore-Ludlow B, Fassl A, Russell CN, Latorre IJ, Jiang B, Graham DB, Perez JR, Sicinski P, Phillips AJ, Schreiber SL, Gray NS, Shamji AF, Xavier RJ. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat Chem Biol. 2017 Oct; 13(10):1102-1108.
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Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS. Characterization of a highly selective inhibitor of the Aurora kinases. Bioorg Med Chem Lett. 2017 09 15; 27(18):4405-4408.
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Zeng M, Lu J, Li L, Feru F, Quan C, Gero TW, Ficarro SB, Xiong Y, Ambrogio C, Paranal RM, Catalano M, Shao J, Wong KK, Marto JA, Fischer ES, Jänne PA, Scott DA, Westover KD, Gray NS. Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chem Biol. 2017 Aug 17; 24(8):1005-1016.e3.
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Lu J, Harrison RA, Li L, Zeng M, Gondi S, Scott D, Gray NS, Engen JR, Westover KD. KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. Structure. 2017 09 05; 25(9):1442-1448.e3.
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Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM. Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS One. 2017; 12(8):e0181585.
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Liu Y, Li Y, Wang X, Liu F, Gao P, Quinn MM, Li F, Merlino AA, Benes C, Liu Q, Gray NS, Wong KK. Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma. Cancer Res. 2017 09 15; 77(18):5068-5076.
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Weir MC, Hellwig S, Tan L, Liu Y, Gray NS, Smithgall TE. Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth. PLoS One. 2017; 12(7):e0181178.
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Winter GE, Mayer A, Buckley DL, Erb MA, Roderick JE, Vittori S, Reyes JM, di Iulio J, Souza A, Ott CJ, Roberts JM, Zeid R, Scott TG, Paulk J, Lachance K, Olson CM, Dastjerdi S, Bauer S, Lin CY, Gray NS, Kelliher MA, Churchman LS, Bradner JE. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 06; 67(1):5-18.e19.
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Mujahid N, Liang Y, Murakami R, Choi HG, Dobry AS, Wang J, Suita Y, Weng QY, Allouche J, Kemeny LV, Hermann AL, Roider EM, Gray NS, Fisher DE. A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. Cell Rep. 2017 06 13; 19(11):2177-2184.
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Wang B, Deng Y, Chen Y, Yu K, Wang A, Liang Q, Wang W, Chen C, Wu H, Hu C, Miao W, Hur W, Wang W, Hu Z, Weisberg EL, Wang J, Ren T, Wang Y, Gray NS, Liu Q, Liu J. Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton’s tyrosine kinase (BTK) irreversible inhibitors. Eur J Med Chem. 2017 Sep 08; 137:545-557.
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Vollmer S, Strickson S, Zhang T, Gray N, Lee KL, Rao VR, Cohen P. The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-like receptor agonists. Biochem J. 2017 06 06; 474(12):2027-2038.
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Sun Y, Alberta JA, Pilarz C, Calligaris D, Chadwick EJ, Ramkissoon SH, Ramkissoon LA, Garcia VM, Mazzola E, Goumnerova L, Kane M, Yao Z, Kieran MW, Ligon KL, Hahn WC, Garraway LA, Rosen N, Gray NS, Agar NY, Buhrlage SJ, Segal RA, Stiles CD. A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas. Neuro Oncol. 2017 06 01; 19(6):774-785.
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Zwang Y, Jonas O, Chen C, Rinne ML, Doench JG, Piccioni F, Tan L, Huang HT, Wang J, Ham YJ, O’Connell J, Bhola P, Doshi M, Whitman M, Cima M, Letai A, Root DE, Langer RS, Gray N, Hahn WC. Synergistic interactions with PI3K inhibition that induce apoptosis. Elife. 2017 05 31; 6.
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Williams CAC, Gray NS, Findlay GM. A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening. J Vis Exp. 2017 05 12; (123).
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Manier S, Huynh D, Shen YJ, Zhou J, Yusufzai T, Salem KZ, Ebright RY, Shi J, Park J, Glavey SV, Devine WG, Liu CJ, Leleu X, Quesnel B, Roche-Lestienne C, Snyder JK, Brown LE, Gray N, Bradner J, Whitesell L, Porco JA, Ghobrial IM. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Sci Transl Med. 2017 05 10; 9(389).
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Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS. Discovery of a potent dual ALK and EGFR T790M inhibitor. Eur J Med Chem. 2017 Aug 18; 136:497-510.
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Wu H, Huang Q, Qi Z, Chen Y, Wang A, Chen C, Liang Q, Wang J, Chen W, Dong J, Yu K, Hu C, Wang W, Liu X, Deng Y, Wang L, Wang B, Li X, Gray NS, Liu J, Wei W, Liu Q. Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. Sci Rep. 2017 03 28; 7(1):466.
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Majkowska I, Shitomi Y, Ito N, Gray NS, Itoh Y. Discoidin domain receptor 2 mediates collagen-induced activation of membrane-type 1 matrix metalloproteinase in human fibroblasts. J Biol Chem. 2017 04 21; 292(16):6633-6643.
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Wein MN, Liang Y, Goransson O, Sundberg TB, Wang J, Williams EA, O’Meara MJ, Govea N, Beqo B, Nishimori S, Nagano K, Brooks DJ, Martins JS, Corbin B, Anselmo A, Sadreyev R, Wu JY, Sakamoto K, Foretz M, Xavier RJ, Baron R, Bouxsein ML, Gardella TJ, Divieti-Pajevic P, Gray NS, Kronenberg HM. Corrigendum: SIKs control osteocyte responses to parathyroid hormone. Nat Commun. 2017 02 22; 8:14745.
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Cayrol F, Praditsuktavorn P, Fernando TM, Kwiatkowski N, Marullo R, Calvo-Vidal MN, Phillip J, Pera B, Yang SN, Takpradit K, Roman L, Gaudiano M, Crescenzo R, Ruan J, Inghirami G, Zhang T, Cremaschi G, Gray NS, Cerchietti L. Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nat Commun. 2017 02 20; 8:14747.
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Liang Y, de Wispelaere M, Carocci M, Liu Q, Wang J, Yang PL, Gray NS. Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. ACS Med Chem Lett. 2017 Mar 09; 8(3):344-349.
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Cayrol F, Praditsuktavorn P, Fernando TM, Kwiatkowski N, Marullo R, Calvo-Vidal MN, Phillip J, Pera B, Yang SN, Takpradit K, Roman L, Gaudiano M, Crescenzo R, Ruan J, Inghirami G, Zhang T, Cremaschi G, Gray NS, Cerchietti L. THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nat Commun. 2017 01 30; 8:14290.
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Hatcher JM, Choi HG, Alessi DR, Gray NS. Small-Molecule Inhibitors of LRRK2. Adv Neurobiol. 2017; 14:241-264.
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de Wispelaere M, Carocci M, Liang Y, Liu Q, Sun E, Vetter ML, Wang J, Gray NS, Yang PL. Discovery of host-targeted covalent inhibitors of dengue virus. Antiviral Res. 2017 Mar; 139:171-179.
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Xie X, Kaoud TS, Edupuganti R, Zhang T, Kogawa T, Zhao Y, Chauhan GB, Giannoukos DN, Qi Y, Tripathy D, Wang J, Gray NS, Dalby KN, Bartholomeusz C, Ueno NT. c-Jun N-terminal kinase promotes stem cell phenotype in triple-negative breast cancer through upregulation of Notch1 via activation of c-Jun. Oncogene. 2017 05 04; 36(18):2599-2608.
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Tan L, Gurbani D, Weisberg EL, Hunter JC, Li L, Jones DS, Ficarro SB, Mowafy S, Tam CP, Rao S, Du G, Griffin JD, Sorger PK, Marto JA, Westover KD, Gray NS. Structure-guided development of covalent TAK1 inhibitors. Bioorg Med Chem. 2017 02 01; 25(3):838-846.
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Beelontally R, Wilkie GS, Lau B, Goodmaker CJ, Ho CMK, Swanson CM, Deng X, Wang J, Gray NS, Davison AJ, Strang BL. Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins. Antiviral Res. 2017 02; 138:61-67.
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Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G, Nonami A, Griffin JD, Lauffenburger DA, Westover KD, Sorger PK, Gray NS. Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. Bioorg Med Chem. 2017 02 15; 25(4):1320-1328.
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2016

Ficarro SB, Browne CM, Card JD, Alexander WM, Zhang T, Park E, McNally R, Dhe-Paganon S, Seo HS, Lamberto I, Eck MJ, Buhrlage SJ, Gray NS, Marto JA. Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes. Anal Chem. 2016 12 20; 88(24):12248-12254.
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Xiong Y, Lu J, Hunter J, Li L, Scott D, Choi HG, Lim SM, Manandhar A, Gondi S, Sim T, Westover KD, Gray NS. Covalent Guanosine Mimetic Inhibitors of G12C KRAS. ACS Med Chem Lett. 2017 Jan 12; 8(1):61-66.
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Shen Y, Park CS, Suppipat K, Mistretta TA, Puppi M, Horton TM, Rabin K, Gray NS, Meijerink JPP, Lacorazza HD. Inactivation of KLF4 promotes T-cell acute lymphoblastic leukemia and activates the MAP2K7 pathway. Leukemia. 2017 06; 31(6):1314-1324.
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Hur W, Rosen H, Gray NS. A benzo[b]thiophene-based selective type 4 S1P receptor agonist. Bioorg Med Chem Lett. 2017 01 01; 27(1):1-5.
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Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, Gray NS, Weisberg EL, Chen L, Liu J, Yun CH, Liu Q. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. 2016 Oct 25; 7(43):69760-69769.
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Wein MN, Liang Y, Goransson O, Sundberg TB, Wang J, Williams EA, O’Meara MJ, Govea N, Beqo B, Nishimori S, Nagano K, Brooks DJ, Martins JS, Corbin B, Anselmo A, Sadreyev R, Wu JY, Sakamoto K, Foretz M, Xavier RJ, Baron R, Bouxsein ML, Gardella TJ, Divieti-Pajevic P, Gray NS, Kronenberg HM. SIKs control osteocyte responses to parathyroid hormone. Nat Commun. 2016 10 19; 7:13176.
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Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016 10; 12(10):876-84.
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Fan F, He Z, Kong LL, Chen Q, Yuan Q, Zhang S, Ye J, Liu H, Sun X, Geng J, Yuan L, Hong L, Xiao C, Zhang W, Sun X, Li Y, Wang P, Huang L, Wu X, Ji Z, Wu Q, Xia NS, Gray NS, Chen L, Yun CH, Deng X, Zhou D. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 08 17; 8(352):352ra108.
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Wang Y, Begley M, Li Q, Huang HT, Lako A, Eck MJ, Gray NS, Mitchison TJ, Cantley LC, Zhao JJ. Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci U S A. 2016 08 30; 113(35):9810-5.
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Williams CA, Fernandez-Alonso R, Wang J, Toth R, Gray NS, Findlay GM. Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity. Cell Rep. 2016 08 16; 16(7):1820-8.
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Ferguson FM, Ni J, Zhang T, Tesar B, Sim T, Kim ND, Deng X, Brown JR, Zhao JJ, Gray NS. Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-d/? Inhibitors. ACS Med Chem Lett. 2016 Oct 13; 7(10):908-912.
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Miranda F, Mannion D, Liu S, Zheng Y, Mangala LS, Redondo C, Herrero-Gonzalez S, Xu R, Taylor C, Chedom DF, Karaminejadranjbar M, Albukhari A, Jiang D, Pradeep S, Rodriguez-Aguayo C, Lopez-Berestein G, Salah E, Abdul Azeez KR, Elkins JM, Campo L, Myers KA, Klotz D, Bivona S, Dhar S, Bast RC, Saya H, Choi HG, Gray NS, Fischer R, Kessler BM, Yau C, Sood AK, Motohara T, Knapp S, Ahmed AA. Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. Cancer Cell. 2016 08 08; 30(2):273-289.
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Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu MR, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 07 19; 12(8):656.
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Iorio F, Knijnenburg TA, Vis DJ, Bignell GR, Menden MP, Schubert M, Aben N, Gonçalves E, Barthorpe S, Lightfoot H, Cokelaer T, Greninger P, van Dyk E, Chang H, de Silva H, Heyn H, Deng X, Egan RK, Liu Q, Mironenko T, Mitropoulos X, Richardson L, Wang J, Zhang T, Moran S, Sayols S, Soleimani M, Tamborero D, Lopez-Bigas N, Ross-Macdonald P, Esteller M, Gray NS, Haber DA, Stratton MR, Benes CH, Wessels LFA, Saez-Rodriguez J, McDermott U, Garnett MJ. A Landscape of Pharmacogenomic Interactions in Cancer. Cell. 2016 Jul 28; 166(3):740-754.
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Chong CR, Bahcall M, Capelletti M, Kosaka T, Ercan D, Sim T, Sholl LM, Nishino M, Johnson BE, Gray NS, Jänne PA. Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer. Clin Cancer Res. 2017 Jan 01; 23(1):204-213.
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Brown WS, Tan L, Smith A, Gray NS, Wendt MK. Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer. . 2016 09; 15(9):2096-106.
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Lee S, Shang Y, Redmond SA, Urisman A, Tang AA, Li KH, Burlingame AL, Pak RA, Jovicic A, Gitler AD, Wang J, Gray NS, Seeley WW, Siddique T, Bigio EH, Lee VM, Trojanowski JQ, Chan JR, Huang EJ. Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis. Neuron. 2016 07 06; 91(1):41-55.
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Sundberg TB, Liang Y, Wu H, Choi HG, Kim ND, Sim T, Johannessen L, Petrone A, Khor B, Graham DB, Latorre IJ, Phillips AJ, Schreiber SL, Perez J, Shamji AF, Gray NS, Xavier RJ. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 08 19; 11(8):2105-11.
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Matthews JM, Bhatt S, Patricelli MP, Nomanbhoy TK, Jiang X, Natkunam Y, Gentles AJ, Martinez E, Zhu D, Chapman JR, Cortizas E, Shyam R, Chinichian S, Advani R, Tan L, Zhang J, Choi HG, Tibshirani R, Buhrlage SJ, Gratzinger D, Verdun R, Gray NS, Lossos IS. Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. Blood. 2016 07 14; 128(2):239-48.
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Yang G, Buhrlage SJ, Tan L, Liu X, Chen J, Xu L, Tsakmaklis N, Chen JG, Patterson CJ, Brown JR, Castillo JJ, Zhang W, Zhang X, Liu S, Cohen P, Hunter ZR, Gray N, Treon SP. HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. Blood. 2016 06 23; 127(25):3237-52.
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Udayakumar D, Pandita RK, Horikoshi N, Liu Y, Liu Q, Wong KK, Hunt CR, Gray NS, Minna JD, Pandita TK, Westover KD. Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair. Radiat Res. 2016 05; 185(5):527-38.
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Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 06; 12(6):452-8.
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Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W, Zhao Z, Wang A, Chen Y, Wang L, Gray NS, Liu J, Zhang X, Liu Q. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 06 17; 11(6):1537-43.
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Clark MJ, Miduturu C, Schmidt AG, Zhu X, Pitts JD, Wang J, Potisopon S, Zhang J, Wojciechowski A, Hann Chu JJ, Gray NS, Yang PL. GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Cell Chem Biol. 2016 04 21; 23(4):443-52.
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Liu X, Hunter ZR, Xu L, Chen J, Chen JG, Tsakmaklis N, Patterson CJ, Castillo JJ, Buhrlage S, Gray N, Treon SP, Yang G. Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia. Br J Haematol. 2017 06; 177(5):808-813.
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Hatcher JM, Weisberg E, Sim T, Stone RM, Liu S, Griffin JD, Gray NS. Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. ACS Med Chem Lett. 2016 May 12; 7(5):476-81.
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Ho CM, Donovan-Banfield IZ, Tan L, Zhang T, Gray NS, Strang BL. Inhibition of IKKa by BAY61-3606 Reveals IKKa-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells. PLoS One. 2016; 11(3):e0150339.
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Westover KD, Jänne PA, Gray NS. Progress on Covalent Inhibition of KRAS(G12C). Cancer Discov. 2016 Mar; 6(3):233-4.
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Nishikawa JL, Boeszoermenyi A, Vale-Silva LA, Torelli R, Posteraro B, Sohn YJ, Ji F, Gelev V, Sanglard D, Sanguinetti M, Sadreyev RI, Mukherjee G, Bhyravabhotla J, Buhrlage SJ, Gray NS, Wagner G, Näär AM, Arthanari H. Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature. 2016 Feb 25; 530(7591):485-9.
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Ye S, Zhang J, Shen J, Gao Y, Li Y, Choy E, Cote G, Harmon D, Mankin H, Gray NS, Hornicek FJ, Duan Z. NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (PGP1) function. Br J Pharmacol. 2016 Feb; 173(3):613-26.
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Amato KR, Wang S, Tan L, Hastings AK, Song W, Lovly CM, Meador CB, Ye F, Lu P, Balko JM, Colvin DC, Cates JM, Pao W, Gray NS, Chen J. EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Res. 2016 Jan 15; 76(2):305-18.
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Neel VA, Todorova K, Wang J, Kwon E, Kang M, Liu Q, Gray N, Lee SW, Mandinova A. Sustained Akt Activity Is Required to Maintain Cell Viability in Seborrheic Keratosis, a Benign Epithelial Tumor. J Invest Dermatol. 2016 Mar; 136(3):696-705.
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Maxson JE, Abel ML, Wang J, Deng X, Reckel S, Luty SB, Sun H, Gorenstein J, Hughes SB, Bottomly D, Wilmot B, McWeeney SK, Radich J, Hantschel O, Middleton RE, Gray NS, Druker BJ, Tyner JW. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2016 Jan 01; 76(1):127-38.
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Debruyne DN, Bhatnagar N, Sharma B, Luther W, Moore NF, Cheung NK, Gray NS, George RE. ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT. Oncogene. 2016 07 14; 35(28):3681-91.
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2015

Hatcher JM, Bahcall M, Choi HG, Gao Y, Sim T, George R, Jänne PA, Gray NS. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10; 58(23):9296-9308.
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Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O’Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. Corrigendum: The promise and peril of chemical probes. Nat Chem Biol. 2015 Nov; 11(11):887.
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Müller S, Chaikuad A, Gray NS, Knapp S. The ins and outs of selective kinase inhibitor development. Nat Chem Biol. 2015 Nov; 11(11):818-21.
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Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, Zhao P, Wang J, Wang C, Weisberg EL, Gray NS, Yun CH, Liu J, Chen L, Liu Q. Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. Oncotarget. 2015 Oct 13; 6(31):31313-22.
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Galli GG, Carrara M, Yuan WC, Valdes-Quezada C, Gurung B, Pepe-Mooney B, Zhang T, Geeven G, Gray NS, de Laat W, Calogero RA, Camargo FD. YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers. Mol Cell. 2015 Oct 15; 60(2):328-37.
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Terai H, Tan L, Beauchamp EM, Hatcher JM, Liu Q, Meyerson M, Gray NS, Hammerman PS. Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer. ACS Chem Biol. 2015 Dec 18; 10(12):2687-96.
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Wang Y, Zhang T, Kwiatkowski N, Abraham BJ, Lee TI, Xie S, Yuzugullu H, Von T, Li H, Lin Z, Stover DG, Lim E, Wang ZC, Iglehart JD, Young RA, Gray NS, Zhao JJ. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015 Sep 24; 163(1):174-86.
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Wilhelmsen K, Xu F, Farrar K, Tran A, Khakpour S, Sundar S, Prakash A, Wang J, Gray NS, Hellman J. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25; 8(391):ra86.
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Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella K, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, Look TA, Arthur JS, Eck MJ, Gray NS. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27; 58(16):6589-606.
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Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O’Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. The promise and peril of chemical probes. Nat Chem Biol. 2015 Aug; 11(8):536-41.
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Wu H, Hu C, Wang A, Weisberg EL, Chen Y, Yun CH, Wang W, Liu Y, Liu X, Tian B, Wang J, Zhao Z, Liang Y, Li B, Wang L, Wang B, Chen C, Buhrlage SJ, Qi Z, Zou F, Nonami A, Li Y, Fernandes SM, Adamia S, Stone RM, Galinsky IA, Wang X, Yang G, Griffin JD, Brown JR, Eck MJ, Liu J, Gray NS, Liu Q. Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. Leukemia. 2016 Jan; 30(1):173-81.
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Rubinow KB, Wang S, den Hartigh LJ, Subramanian S, Morton GJ, Buaas FW, Lamont D, Gray N, Braun RE, Page ST. Hematopoietic androgen receptor deficiency promotes visceral fat deposition in male mice without impairing glucose homeostasis. Andrology. 2015 Jul; 3(4):787-96.
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Moccia M, Liu Q, Guida T, Federico G, Brescia A, Zhao Z, Choi HG, Deng X, Tan L, Wang J, Billaud M, Gray NS, Carlomagno F, Santoro M. Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. PLoS One. 2015; 10(6):e0128364.
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Tricker EM, Xu C, Uddin S, Capelletti M, Ercan D, Ogino A, Pratilas CA, Rosen N, Gray NS, Wong KK, Jänne PA. Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer. Cancer Discov. 2015 Sep; 5(9):960-971.
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Wang J, Gray NS. SnapShot: Kinase Inhibitors I. Mol Cell. 2015 May 21; 58(4):708.e1.
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Wang J, Gray NS. SnapShot: Kinase Inhibitors II. Mol Cell. 2015 May 21; 58(4):710.e1.
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Lim SM, Xie T, Westover KD, Ficarro SB, Tae HS, Gurbani D, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Development of small molecules targeting the pseudokinase Her3. Bioorg Med Chem Lett. 2015 Aug 15; 25(16):3382-9.
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Ercan D, Choi HG, Yun CH, Capelletti M, Xie T, Eck MJ, Gray NS, Jänne PA. EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors. Clin Cancer Res. 2015 Sep 01; 21(17):3913-23.
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Malik N, Vollmer S, Nanda SK, Lopez-Pelaez M, Prescott A, Gray N, Cohen P. Suppression of interferon ß gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15; 468(3):363-72.
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Hatcher JM, Zhang J, Choi HG, Ito G, Alessi DR, Gray NS. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 May 14; 6(5):584-9.
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Nonami A, Sattler M, Weisberg E, Liu Q, Zhang J, Patricelli MP, Christie AL, Saur AM, Kohl NE, Kung AL, Yoon H, Sim T, Gray NS, Griffin JD. Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. Blood. 2015 May 14; 125(20):3133-43.
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Fallahi-Sichani M, Moerke NJ, Niepel M, Zhang T, Gray NS, Sorger PK. Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. Mol Syst Biol. 2015 Mar 26; 11(3):797.
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Miao B, Ji Z, Tan L, Taylor M, Zhang J, Choi HG, Frederick DT, Kumar R, Wargo JA, Flaherty KT, Gray NS, Tsao H. EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma. Cancer Discov. 2015 Mar; 5(3):274-87.
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2014

Christensen CL, Kwiatkowski N, Abraham BJ, Carretero J, Al-Shahrour F, Zhang T, Chipumuro E, Herter-Sprie GS, Akbay EA, Altabef A, Zhang J, Shimamura T, Capelletti M, Reibel JB, Cavanaugh JD, Gao P, Liu Y, Michaelsen SR, Poulsen HS, Aref AR, Barbie DA, Bradner JE, George RE, Gray NS, Young RA, Wong KK. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014 Dec 08; 26(6):909-922.
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Moroco JA, Baumgartner MP, Rust HL, Choi HG, Hur W, Gray NS, Camacho CJ, Smithgall TE. A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region. Chem Biol Drug Des. 2015 Aug; 86(2):144-55.
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Chipumuro E, Marco E, Christensen CL, Kwiatkowski N, Zhang T, Hatheway CM, Abraham BJ, Sharma B, Yeung C, Altabef A, Perez-Atayde A, Wong KK, Yuan GC, Gray NS, Young RA, George RE. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20; 159(5):1126-1139.
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Umapathy G, El Wakil A, Witek B, Chesler L, Danielson L, Deng X, Gray NS, Johansson M, Kvarnbrink S, Ruuth K, Schönherr C, Palmer RH, Hallberg B. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28; 7(349):ra102.
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Huang Z, Tan L, Wang H, Liu Y, Blais S, Deng J, Neubert TA, Gray NS, Li X, Mohammadi M. DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors. ACS Chem Biol. 2015 Jan 16; 10(1):299-309.
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Tan L, Wang J, Tanizaki J, Huang Z, Aref AR, Rusan M, Zhu SJ, Zhang Y, Ercan D, Liao RG, Capelletti M, Zhou W, Hur W, Kim N, Sim T, Gaudet S, Barbie DA, Yeh JR, Yun CH, Hammerman PS, Mohammadi M, Jänne PA, Gray NS. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11; 111(45):E4869-77.
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Xie T, Lim SM, Westover KD, Dodge ME, Ercan D, Ficarro SB, Udayakumar D, Gurbani D, Tae HS, Riddle SM, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Pharmacological targeting of the pseudokinase Her3. Nat Chem Biol. 2014 Dec; 10(12):1006-12.
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Lopez-Pelaez M, Lamont DJ, Peggie M, Shpiro N, Gray NS, Cohen P. Protein kinase IKKß-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells. Proc Natl Acad Sci U S A. 2014 Dec 09; 111(49):17432-7.
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Wagle N, Grabiner BC, Van Allen EM, Amin-Mansour A, Taylor-Weiner A, Rosenberg M, Gray N, Barletta JA, Guo Y, Swanson SJ, Ruan DT, Hanna GJ, Haddad RI, Getz G, Kwiatkowski DJ, Carter SL, Sabatini DM, Jänne PA, Garraway LA, Lorch JH. Response and acquired resistance to everolimus in anaplastic thyroid cancer. N Engl J Med. 2014 Oct 09; 371(15):1426-33.
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Theunissen TW, Powell BE, Wang H, Mitalipova M, Faddah DA, Reddy J, Fan ZP, Maetzel D, Ganz K, Shi L, Lungjangwa T, Imsoonthornruksa S, Stelzer Y, Rangarajan S, D’Alessio A, Zhang J, Gao Q, Dawlaty MM, Young RA, Gray NS, Jaenisch R. Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 2014 Oct 02; 15(4):524-526.
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Moore NF, Azarova AM, Bhatnagar N, Ross KN, Drake LE, Frumm S, Liu QS, Christie AL, Sanda T, Chesler L, Kung AL, Gray NS, Stegmaier K, George RE. Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma. Oncotarget. 2014 Sep 30; 5(18):8737-49.
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Duan Z, Zhang J, Ye S, Shen J, Choy E, Cote G, Harmon D, Mankin H, Hua Y, Zhang Y, Gray NS, Hornicek FJ. A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells. BMC Cancer. 2014 Sep 19; 14:681.
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Chaikuad A, Tacconi EM, Zimmer J, Liang Y, Gray NS, Tarsounas M, Knapp S. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol. 2014 Oct; 10(10):853-60.
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Weisberg E, Nonami A, Chen Z, Nelson E, Chen Y, Liu F, Cho H, Zhang J, Sattler M, Mitsiades C, Wong KK, Liu Q, Gray NS, Griffin JD. Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clin Cancer Res. 2014 Nov 01; 20(21):5483-95.
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Rovida E, Di Maira G, Tusa I, Cannito S, Paternostro C, Navari N, Vivoli E, Deng X, Gray NS, Esparís-Ogando A, David E, Pandiella A, Dello Sbarba P, Parola M, Marra F. The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma. Gut. 2015 Sep; 64(9):1454-65.
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Calles A, Kwiatkowski N, Cammarata BK, Ercan D, Gray NS, Jänne PA. Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines. Mol Oncol. 2015 Jan; 9(1):260-9.
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Ritorto MS, Ewan R, Perez-Oliva AB, Knebel A, Buhrlage SJ, Wightman M, Kelly SM, Wood NT, Virdee S, Gray NS, Morrice NA, Alessi DR, Trost M. Screening of DUB activity and specificity by MALDI-TOF mass spectrometry. Nat Commun. 2014 Aug 27; 5:4763.
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Theunissen TW, Powell BE, Wang H, Mitalipova M, Faddah DA, Reddy J, Fan ZP, Maetzel D, Ganz K, Shi L, Lungjangwa T, Imsoonthornruksa S, Stelzer Y, Rangarajan S, D’Alessio A, Zhang J, Gao Q, Dawlaty MM, Young RA, Gray NS, Jaenisch R. Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 2014 Oct 02; 15(4):523.
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Sundberg TB, Choi HG, Song JH, Russell CN, Hussain MM, Graham DB, Khor B, Gagnon J, O’Connell DJ, Narayan K, Dancík V, Perez JR, Reinecker HC, Gray NS, Schreiber SL, Xavier RJ, Shamji AF. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proc Natl Acad Sci U S A. 2014 Aug 26; 111(34):12468-73.
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Derbyshire ER, Zuzarte-Luís V, Magalhães AD, Kato N, Sanschagrin PC, Wang J, Zhou W, Miduturu CV, Mazitschek R, Sliz P, Mota MM, Gray NS, Clardy J. Chemical interrogation of the malaria kinome. Chembiochem. 2014 Sep 05; 15(13):1920-30.
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Patel K, Foretz M, Marion A, Campbell DG, Gourlay R, Boudaba N, Tournier E, Titchenell P, Peggie M, Deak M, Wan M, Kaestner KH, Göransson O, Viollet B, Gray NS, Birnbaum MJ, Sutherland C, Sakamoto K. The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nat Commun. 2014 Aug 04; 5:4535.
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Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y, Choi HG, Xie T, Deng X, Buhrlage SJ, Sim T, Cohen P, Sapkota G, Westover KD, Gray NS. Discovery of type II inhibitors of TGFß-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 08; 58(1):183-96.
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Theunissen TW, Powell BE, Wang H, Mitalipova M, Faddah DA, Reddy J, Fan ZP, Maetzel D, Ganz K, Shi L, Lungjangwa T, Imsoonthornruksa S, Stelzer Y, Rangarajan S, D’Alessio A, Zhang J, Gao Q, Dawlaty MM, Young RA, Gray NS, Jaenisch R. Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell. 2014 10 02; 15(4):471-487.
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Murchie P, Raja EA, Brewster DH, Campbell NC, Ritchie LD, Robertson R, Samuel L, Gray N, Lee AJ. Time from first presentation in primary care to treatment of symptomatic colorectal cancer: effect on disease stage and survival. Br J Cancer. 2014 Jul 29; 111(3):461-9.
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Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31; 511(7511):616-20.
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Wang J, Mikse O, Liao RG, Li Y, Tan L, Janne PA, Gray NS, Wong KK, Hammerman PS. Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells. Oncogene. 2015 Apr 23; 34(17):2167-77.
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Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, Xie T, Marto JA, Chen Z, Gray NS, Westover KD. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014 Jun 17; 111(24):8895-900.
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Wang Y, Lee YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ. MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 2014 May 20; 3:e01763.
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Vetter ML, Zhang Z, Liu S, Wang J, Cho H, Zhang J, Zhang W, Gray NS, Yang PL. Fluorescent visualization of Src by using dasatinib-BODIPY. Chembiochem. 2014 Jun 16; 15(9):1317-24.
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Weisberg E, Nonami A, Chen Z, Liu F, Zhang J, Sattler M, Nelson E, Cowens K, Christie AL, Mitsiades C, Wong KK, Liu Q, Gray N, Griffin JD. Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies. Leukemia. 2015 Jan; 29(1):27-37.
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Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS. Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem Biol. 2014 Jun 20; 9(6):1230-41.
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Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN. Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors. J Mol Biol. 2014 Jun 26; 426(13):2457-70.
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Amato KR, Wang S, Hastings AK, Youngblood VM, Santapuram PR, Chen H, Cates JM, Colvin DC, Ye F, Brantley-Sieders DM, Cook RS, Tan L, Gray NS, Chen J. Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. J Clin Invest. 2014 May; 124(5):2037-49.
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Codeluppi S, Fernandez-Zafra T, Sandor K, Kjell J, Liu Q, Abrams M, Olson L, Gray NS, Svensson CI, Uhlén P. Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. PLoS One. 2014; 9(3):e92649.
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Decker S, Finter J, Forde AJ, Kissel S, Schwaller J, Mack TS, Kuhn A, Gray N, Follo M, Jumaa H, Burger M, Zirlik K, Pfeifer D, Miduturu CV, Eibel H, Veelken H, Dierks C. PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1). . 2014 May; 13(5):1231-45.
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Wu H, Wang W, Liu F, Weisberg EL, Tian B, Chen Y, Li B, Wang A, Wang B, Zhao Z, McMillin DW, Hu C, Li H, Wang J, Liang Y, Buhrlage SJ, Liang J, Liu J, Yang G, Brown JR, Treon SP, Mitsiades CS, Griffin JD, Liu Q, Gray NS. Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma. ACS Chem Biol. 2014 May 16; 9(5):1086-91.
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Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell S, Zhao Z, Wu H, Wang J, Mandinova A, Bullock AN, Liu Q, Lee SW, Gray NS. Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor. ACS Chem Biol. 2014 Mar 21; 9(3):840.
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Ficarro SB, Biagi JM, Wang J, Scotcher J, Koleva RI, Card JD, Adelmant G, He H, Askenazi M, Marshall AG, Young NL, Gray NS, Marto JA. Protected amine labels: a versatile molecular scaffold for multiplexed nominal mass and sub-Da isotopologue quantitative proteomic reagents. J Am Soc Mass Spectrom. 2014 Apr; 25(4):636-50.
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Gray NS, Fabbro D. Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. Methods Enzymol. 2014; 548:173-88.
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Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 01; 457(1):215-25.
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Beauchamp EM, Woods BA, Dulak AM, Tan L, Xu C, Gray NS, Bass AJ, Wong KK, Meyerson M, Hammerman PS. Acquired resistance to dasatinib in lung cancer cell lines conferred by DDR2 gatekeeper mutation and NF1 loss. . 2014 Feb; 13(2):475-82.
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Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, Carrasco M, Hunter J, Kim ND, Xie T, Sim T, Jänne PA, Meyerson M, Marto JA, Engen JR, Gray NS. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014 Jan 03; 53(1):199-204.
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2013

Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013; 70:758-67.
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Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D’Andrea AD, Parmar K. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. . 2013 Dec; 12(12):2651-62.
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Angell HK, Gray N, Womack C, Pritchard DI, Wilkinson RW, Cumberbatch M. Digital pattern recognition-based image analysis quantifies immune infiltrates in distinct tissue regions of colorectal cancer and identifies a metastatic phenotype. Br J Cancer. 2013 Sep 17; 109(6):1618-24.
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Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell SA, Wu H, Zhao Z, Wang J, Mandinova A, Griffin JD, Bullock AN, Liu Q, Lee SW, Gray NS. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18; 8(10):2145-50.
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Tannous BA, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, Geerts D, De Witt Hamer PC, Hagemann C, Vandertop WP, Van Tellingen O, Noske DP, Gray NS, Würdinger T. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 04; 105(17):1322-31.
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Kang SA, Pacold ME, Cervantes CL, Lim D, Lou HJ, Ottina K, Gray NS, Turk BE, Yaffe MB, Sabatini DM. mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science. 2013 Jul 26; 341(6144):1236566.
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Yang G, Zhou Y, Liu X, Xu L, Cao Y, Manning RJ, Patterson CJ, Buhrlage SJ, Gray N, Tai YT, Anderson KC, Hunter ZR, Treon SP. A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia. Blood. 2013 Aug 15; 122(7):1222-32.
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Taipale M, Krykbaeva I, Whitesell L, Santagata S, Zhang J, Liu Q, Gray NS, Lindquist S. Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells. Nat Biotechnol. 2013 Jul; 31(7):630-7.
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Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25; 56(14):5675-90.
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Liao RG, Jung J, Tchaicha J, Wilkerson MD, Sivachenko A, Beauchamp EM, Liu Q, Pugh TJ, Pedamallu CS, Hayes DN, Gray NS, Getz G, Wong KK, Haddad RI, Meyerson M, Hammerman PS. Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. Cancer Res. 2013 Aug 15; 73(16):5195-205.
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Liu Y, Marks K, Cowley GS, Carretero J, Liu Q, Nieland TJ, Xu C, Cohoon TJ, Gao P, Zhang Y, Chen Z, Altabef AB, Tchaicha JH, Wang X, Choe S, Driggers EM, Zhang J, Bailey ST, Sharpless NE, Hayes DN, Patel NM, Janne PA, Bardeesy N, Engelman JA, Manning BD, Shaw RJ, Asara JM, Scully R, Kimmelman A, Byers LA, Gibbons DL, Wistuba II, Heymach JV, Kwiatkowski DJ, Kim WY, Kung AL, Gray NS, Root DE, Cantley LC, Wong KK. Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. Cancer Discov. 2013 Aug; 3(8):870-9.
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Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J Med Chem. 2013 Jun 13; 56(11):4413-21.
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Liu F, Zhang X, Weisberg E, Chen S, Hur W, Wu H, Zhao Z, Wang W, Mao M, Cai C, Simon NI, Sanda T, Wang J, Look AT, Griffin JD, Balk SP, Liu Q, Gray NS. Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol. 2013 Jul 19; 8(7):1423-8.
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Guo Y, Chekaluk Y, Zhang J, Du J, Gray NS, Wu CL, Kwiatkowski DJ. TSC1 involvement in bladder cancer: diverse effects and therapeutic implications. J Pathol. 2013 May; 230(1):17-27.
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Jain R, Jain D, Liu Q, Bartosinska B, Wang J, Schumann D, Kauschke SG, Eickelmann P, Piemonti L, Gray NS, Lammert E. Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets. Diabetologia. 2013 Jun; 56(6):1350-5.
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Sanda T, Tyner JW, Gutierrez A, Ngo VN, Glover J, Chang BH, Yost A, Ma W, Fleischman AG, Zhou W, Yang Y, Kleppe M, Ahn Y, Tatarek J, Kelliher MA, Neuberg DS, Levine RL, Moriggl R, Müller M, Gray NS, Jamieson CH, Weng AP, Staudt LM, Druker BJ, Look AT. TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discov. 2013 May; 3(5):564-77.
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Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Res. 2013 Apr 15; 73(8):2574-86.
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Weisberg E, Liu Q, Zhang X, Nelson E, Sattler M, Liu F, Nicolais M, Zhang J, Mitsiades C, Smith RW, Stone R, Galinsky I, Nonami A, Griffin JD, Gray N. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013; 8(2):e56473.
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Liu Q, Sabnis Y, Zhao Z, Zhang T, Buhrlage SJ, Jones LH, Gray NS. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. 2013 Feb 21; 20(2):146-59.
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Pan S, Gray NS, Gao W, Mi Y, Fan Y, Wang X, Tuntland T, Che J, Lefebvre S, Chen Y, Chu A, Hinterding K, Gardin A, End P, Heining P, Bruns C, Cooke NG, Nuesslein-Hildesheim B. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Mar 14; 4(3):333-7.
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Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ. A public-private partnership to unlock the untargeted kinome. Nat Chem Biol. 2013 Jan; 9(1):3-6.
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Cortot AB, Repellin CE, Shimamura T, Capelletti M, Zejnullahu K, Ercan D, Christensen JG, Wong KK, Gray NS, Jänne PA. Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer Res. 2013 Jan 15; 73(2):834-43.
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2012

Deng X, Choi HG, Buhrlage SJ, Gray NS. Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 – 2011). Expert Opin Ther Pat. 2012 Dec; 22(12):1415-26.
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Gergely P, Nuesslein-Hildesheim B, Guerini D, Brinkmann V, Traebert M, Bruns C, Pan S, Gray NS, Hinterding K, Cooke NG, Groenewegen A, Vitaliti A, Sing T, Luttringer O, Yang J, Gardin A, Wang N, Crumb WJ, Saltzman M, Rosenberg M, Wallström E. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov; 167(5):1035-47.
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Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E, Gray NS, Arthur JS, Cohen P. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16; 109(42):16986-91.
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Zhang Z, Kwiatkowski N, Zeng H, Lim SM, Gray NS, Zhang W, Yang PL. Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy. Mol Biosyst. 2012 Oct; 8(10):2523-6.
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Ercan D, Xu C, Yanagita M, Monast CS, Pratilas CA, Montero J, Butaney M, Shimamura T, Sholl L, Ivanova EV, Tadi M, Rogers A, Repellin C, Capelletti M, Maertens O, Goetz EM, Letai A, Garraway LA, Lazzara MJ, Rosen N, Gray NS, Wong KK, Jänne PA. Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov. 2012 Oct; 2(10):934-47.
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Yang Q, Liao L, Deng X, Chen R, Gray NS, Yates JR, Lee JD. BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction. Oncogene. 2013 Jun 27; 32(26):3156-64.
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Lau KS, Zhang T, Kendall KR, Lauffenburger D, Gray NS, Haigis KM. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012; 7(7):e41343.
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Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31; 109(31):12722-7.
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Duan Z, Zhang J, Choy E, Harmon D, Liu X, Nielsen P, Mankin H, Gray NS, Hornicek FJ. Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation. Clin Cancer Res. 2012 Sep 01; 18(17):4580-8.
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Berry T, Luther W, Bhatnagar N, Jamin Y, Poon E, Sanda T, Pei D, Sharma B, Vetharoy WR, Hallsworth A, Ahmad Z, Barker K, Moreau L, Webber H, Wang W, Liu Q, Perez-Atayde A, Rodig S, Cheung NK, Raynaud F, Hallberg B, Robinson SP, Gray NS, Pearson AD, Eccles SA, Chesler L, George RE. The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell. 2012 Jul 10; 22(1):117-30.
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Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Sep 01; 22(17):5625-9.
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Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS. Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases. Bioorg Med Chem Lett. 2012 Aug 15; 22(16):5297-302.
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Dzamko N, Inesta-Vaquera F, Zhang J, Xie C, Cai H, Arthur S, Tan L, Choi H, Gray N, Cohen P, Pedrioli P, Clark K, Alessi DR. The IkappaB kinase family phosphorylates the Parkinson’s disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS One. 2012; 7(6):e39132.
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Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 09; 3(8):658-662.
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Deng X, Zhou W, Weisberg E, Wang J, Zhang J, Sasaki T, Nelson E, Griffin JD, Jänne PA, Gray NS. An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRa and kit. Bioorg Med Chem Lett. 2012 Jul 15; 22(14):4579-84.
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Thoreen CC, Chantranupong L, Keys HR, Wang T, Gray NS, Sabatini DM. A unifying model for mTORC1-mediated regulation of mRNA translation. Nature. 2012 May 02; 485(7396):109-13.
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Hellwig S, Miduturu CV, Kanda S, Zhang J, Filippakopoulos P, Salah E, Deng X, Choi HG, Zhou W, Hur W, Knapp S, Gray NS, Smithgall TE. Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chem Biol. 2012 Apr 20; 19(4):529-40.
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Liu Q, Ren T, Fresques T, Oppliger W, Niles BJ, Hur W, Sabatini DM, Hall MN, Powers T, Gray NS. Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. ACS Chem Biol. 2012 Jun 15; 7(6):982-7.
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Ni J, Liu Q, Xie S, Carlson C, Von T, Vogel K, Riddle S, Benes C, Eck M, Roberts T, Gray N, Zhao J. Functional characterization of an isoform-selective inhibitor of PI3K-p110ß as a potential anticancer agent. Cancer Discov. 2012 May; 2(5):425-33.
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Weisberg E, Liu Q, Nelson E, Kung AL, Christie AL, Bronson R, Sattler M, Sanda T, Zhao Z, Hur W, Mitsiades C, Smith R, Daley JF, Stone R, Galinsky I, Griffin JD, Gray N. Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. Leukemia. 2012 Oct; 26(10):2233-44.
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Garnett MJ, Edelman EJ, Heidorn SJ, Greenman CD, Dastur A, Lau KW, Greninger P, Thompson IR, Luo X, Soares J, Liu Q, Iorio F, Surdez D, Chen L, Milano RJ, Bignell GR, Tam AT, Davies H, Stevenson JA, Barthorpe S, Lutz SR, Kogera F, Lawrence K, McLaren-Douglas A, Mitropoulos X, Mironenko T, Thi H, Richardson L, Zhou W, Jewitt F, Zhang T, O’Brien P, Boisvert JL, Price S, Hur W, Yang W, Deng X, Butler A, Choi HG, Chang JW, Baselga J, Stamenkovic I, Engelman JA, Sharma SV, Delattre O, Saez-Rodriguez J, Gray NS, Settleman J, Futreal PA, Haber DA, Stratton MR, Ramaswamy S, McDermott U, Benes CH. Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature. 2012 Mar 28; 483(7391):570-5.
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Zhang J, Deng X, Choi HG, Alessi DR, Gray NS. Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Mar 01; 22(5):1864-9.
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Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27; 19(1):140-54.
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Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, Kang SA, Zhao J, Look AT, Sorger PK, Sabatini DM, Gray NS. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J Biol Chem. 2012 Mar 23; 287(13):9742-52.
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Liu Q, Kang SA, Thoreen CC, Hur W, Wang J, Chang JW, Markhard A, Zhang J, Sim T, Sabatini DM, Gray NS. Development of ATP-competitive mTOR inhibitors. Methods Mol Biol. 2012; 821:447-60.
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Kwiatkowski N, Deng X, Wang J, Tan L, Villa F, Santaguida S, Huang HC, Mitchison T, Musacchio A, Gray N. Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. ACS Chem Biol. 2012 Jan 20; 7(1):185-96.
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2011

Liu P, Cheng H, Santiago S, Raeder M, Zhang F, Isabella A, Yang J, Semaan DJ, Chen C, Fox EA, Gray NS, Monahan J, Schlegel R, Beroukhim R, Mills GB, Zhao JJ. Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nat Med. 2011 Aug 07; 17(9):1116-20.
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Miduturu CV, Deng X, Kwiatkowski N, Yang W, Brault L, Filippakopoulos P, Chung E, Yang Q, Schwaller J, Knapp S, King RW, Lee JD, Herrgard S, Zarrinkar P, Gray NS. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem Biol. 2011 Jul 29; 18(7):868-79.
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Sasaki T, Koivunen J, Ogino A, Yanagita M, Nikiforow S, Zheng W, Lathan C, Marcoux JP, Du J, Okuda K, Capelletti M, Shimamura T, Ercan D, Stumpfova M, Xiao Y, Weremowicz S, Butaney M, Heon S, Wilner K, Christensen JG, Eck MJ, Wong KK, Lindeman N, Gray NS, Rodig SJ, Jänne PA. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res. 2011 Sep 15; 71(18):6051-60.
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McMillin DW, Delmore J, Negri J, Ooi M, Klippel S, Miduturu CV, Gray NS, Richardson PG, Anderson KC, Kung AL, Mitsiades CS. Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation. PLoS One. 2011; 6(7):e20226.
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Patricelli MP, Nomanbhoy TK, Wu J, Brown H, Zhou D, Zhang J, Jagannathan S, Aban A, Okerberg E, Herring C, Nordin B, Weissig H, Yang Q, Lee JD, Gray NS, Kozarich JW. In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol. 2011 Jun 24; 18(6):699-710.
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Hsu PP, Kang SA, Rameseder J, Zhang Y, Ottina KA, Lim D, Peterson TR, Choi Y, Gray NS, Yaffe MB, Marto JA, Sabatini DM. The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science. 2011 Jun 10; 332(6035):1317-22.
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Dutt A, Ramos AH, Hammerman PS, Mermel C, Cho J, Sharifnia T, Chande A, Tanaka KE, Stransky N, Greulich H, Gray NS, Meyerson M. Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One. 2011; 6(6):e20351.
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Hammerman PS, Sos ML, Ramos AH, Xu C, Dutt A, Zhou W, Brace LE, Woods BA, Lin W, Zhang J, Deng X, Lim SM, Heynck S, Peifer M, Simard JR, Lawrence MS, Onofrio RC, Salvesen HB, Seidel D, Zander T, Heuckmann JM, Soltermann A, Moch H, Koker M, Leenders F, Gabler F, Querings S, Ansén S, Brambilla E, Brambilla C, Lorimier P, Brustugun OT, Helland A, Petersen I, Clement JH, Groen H, Timens W, Sietsma H, Stoelben E, Wolf J, Beer DG, Tsao MS, Hanna M, Hatton C, Eck MJ, Janne PA, Johnson BE, Winckler W, Greulich H, Bass AJ, Cho J, Rauh D, Gray NS, Wong KK, Haura EB, Thomas RK, Meyerson M. Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov. 2011 Jun; 1(1):78-89.
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Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Choi HG, Waller DL, Sim T, Sabatini DM, Gray NS. Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. Bioorg Med Chem Lett. 2011 Jul 01; 21(13):4036-40.
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Haber DA, Gray NS, Baselga J. The evolving war on cancer. Cell. 2011 Apr 01; 145(1):19-24.
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Deng X, Wang J, Zhang J, Sim T, Kim ND, Sasaki T, Luther W, George RE, Jänne PA, Gray NS. Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. ACS Med Chem Lett. 2011 May 12; 2(5):379-384.
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Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR, Gray NS. Characterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2. Nat Chem Biol. 2011 Apr; 7(4):203-5.
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Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem. 2011 Mar 10; 54(5):1473-80.
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Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS. Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1. ACS Med Chem Lett. 2011 Mar 10; 2(3):195-200.
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Iacob RE, Zhang J, Gray NS, Engen JR. Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One. 2011 Jan 10; 6(1):e15929.
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Hur W, Gray NS. Small molecule modulators of antioxidant response pathway. Curr Opin Chem Biol. 2011 Feb; 15(1):162-73.
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Zhou W, Ercan D, Jänne PA, Gray NS. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg Med Chem Lett. 2011 Jan 15; 21(2):638-43.
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2010

Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray NS, Wilner K, Christensen JG, Demetri G, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA. The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res. 2010 Dec 15; 70(24):10038-43.
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Chen Z, Sasaki T, Tan X, Carretero J, Shimamura T, Li D, Xu C, Wang Y, Adelmant GO, Capelletti M, Lee HJ, Rodig SJ, Borgman C, Park SI, Kim HR, Padera R, Marto JA, Gray NS, Kung AL, Shapiro GI, Jänne PA, Wong KK. Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res. 2010 Dec 01; 70(23):9827-36.
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Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14; 53(19):7146-55.
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Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem. 2010 Oct 14; 53(19):6934-46.
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Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR, Gray NS, Lee JD. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010 Sep 14; 18(3):258-67.
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Weisberg E, Choi HG, Barrett R, Zhou W, Zhang J, Ray A, Nelson EA, Jiang J, Moreno D, Stone R, Galinsky I, Fox E, Adamia S, Kung AL, Gray NS, Griffin JD. Discovery and characterization of novel mutant FLT3 kinase inhibitors. . 2010 Sep; 9(9):2468-77.
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Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T. A type-II kinase inhibitor capable of inhibiting the T315I “gatekeeper” mutant of Bcr-Abl. J Med Chem. 2010 Aug 12; 53(15):5439-48.
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Deng X, Nagle A, Wu T, Sakata T, Henson K, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Tully DC, Chatterjee AK, Gray NS. Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. Bioorg Med Chem Lett. 2010 Jul 15; 20(14):4027-31.
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Hur W, Sun Z, Jiang T, Mason DE, Peters EC, Zhang DD, Luesch H, Schultz PG, Gray NS. A small-molecule inducer of the antioxidant response element. Chem Biol. 2010 May 28; 17(5):537-47.
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Weisberg E, Deng X, Choi HG, Barrett R, Adamia S, Ray A, Moreno D, Kung AL, Gray N, Griffin JD. Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML. Leukemia. 2010 Jul; 24(7):1375-8.
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Deng X, Lim SM, Zhang J, Gray NS. Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorg Med Chem Lett. 2010 Jul 15; 20(14):4196-200.
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Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May; 6(5):359-68.
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Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26; 17(3):285-95.
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Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, Sim T, Zhou W, Seeliger M, Cameron M, Azam M, Fletcher JA, Debiec-Rychter M, Mayeda M, Moreno D, Kung AL, Janne PA, Khosravi-Far R, Melo JV, Manley PW, Adamia S, Wu C, Gray N, Griffin JD. Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants. Blood. 2010 May 27; 115(21):4206-16.
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Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J. Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochim Biophys Acta. 2010 Mar; 1804(3):454-62.
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McDermott U, Pusapati RV, Christensen JG, Gray NS, Settleman J. Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res. 2010 Feb 15; 70(4):1625-34.
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Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28; 463(7280):501-6.
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2009

Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24; 462(7276):1070-4.
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Emery CM, Vijayendran KG, Zipser MC, Sawyer AM, Niu L, Kim JJ, Hatton C, Chopra R, Oberholzer PA, Karpova MB, MacConaill LE, Zhang J, Gray NS, Sellers WR, Dummer R, Garraway LA. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A. 2009 Dec 01; 106(48):20411-6.
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Wu T, Nagle A, Sakata T, Henson K, Borboa R, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Deng X, Gray NS, Tully DC, Chatterjee AK. Cell-based optimization of novel benzamides as potential antimalarial leads. Bioorg Med Chem Lett. 2009 Dec 15; 19(24):6970-4.
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Zhang G, Ren P, Gray NS, Sim T, Wang X, Liu Y, Che J, Dong W, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Wang Z, Seidel HM, Karanewsky DS, He Y. Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorg Med Chem Lett. 2009 Dec 01; 19(23):6691-5.
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Choi Y, Seeliger MA, Panjarian SB, Kim H, Deng X, Sim T, Couch B, Koleske AJ, Smithgall TE, Gray NS. N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem. 2009 Oct 16; 284(42):29005-14.
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Jänne PA, Gray N, Settleman J. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov. 2009 Sep; 8(9):709-23.
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Speake G, Klinowska T, Hickinson M, Marshall G, Smith P, Vincent J, Anderton J, Gray N, Smith I, Ogilvie D. Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile. J Clin Oncol. 2009 May 20; 27(15_suppl):11072.
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Weisberg E, Barrett R, Liu Q, Stone R, Gray N, Griffin JD. FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat. 2009 Jun; 12(3):81-9.
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Peterson TR, Laplante M, Thoreen CC, Sancak Y, Kang SA, Kuehl WM, Gray NS, Sabatini DM. DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell. 2009 May 29; 137(5):873-86.
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Choi Y, Syeda F, Walker JR, Finerty PJ, Cuerrier D, Wojciechowski A, Liu Q, Dhe-Paganon S, Gray NS. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Aug 01; 19(15):4467-70.
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Goldsmith M, Avni D, Levy-Rimler G, Mashiach R, Ernst O, Levi M, Webb B, Meijler MM, Gray NS, Rosen H, Zor T. A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages. Immunology. 2009 May; 127(1):103-15.
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Xian W, Pappas L, Pandya D, Selfors LM, Derksen PW, de Bruin M, Gray NS, Jonkers J, Rosen JM, Brugge JS. Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival. Cancer Res. 2009 Mar 15; 69(6):2244-51.
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Sáenz JB, Sun WJ, Chang JW, Li J, Bursulaya B, Gray NS, Haslam DB. Golgicide A reveals essential roles for GBF1 in Golgi assembly and function. Nat Chem Biol. 2009 Mar; 5(3):157-65.
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Avni D, Goldsmith M, Ernst O, Mashiach R, Tuntland T, Meijler MM, Gray NS, Rosen H, Zor T. Modulation of TNFalpha, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages. Immunol Lett. 2009 Mar 24; 123(1):1-8.
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Iacob RE, Pene-Dumitrescu T, Zhang J, Gray NS, Smithgall TE, Engen JR. Conformational disturbance in Abl kinase upon mutation and deregulation. Proc Natl Acad Sci U S A. 2009 Feb 03; 106(5):1386-91.
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Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20; 284(12):8023-32.
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Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discov Today Ther Strateg. 2009; 6(2):47-55.
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Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer. 2009 Jan; 9(1):28-39.
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2008

George RE, Sanda T, Hanna M, Fröhling S, Luther W, Zhang J, Ahn Y, Zhou W, London WB, McGrady P, Xue L, Zozulya S, Gregor VE, Webb TR, Gray NS, Gilliland DG, Diller L, Greulich H, Morris SW, Meyerson M, Look AT. Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature. 2008 Oct 16; 455(7215):975-8.
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Azam M, Seeliger MA, Gray NS, Kuriyan J, Daley GQ. Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol. 2008 Oct; 15(10):1109-18.
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Zhang G, Ren P, Gray NS, Sim T, Liu Y, Wang X, Che J, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Chow D, Martin Seidel H, Karanewsky DS, He Y. Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. Bioorg Med Chem Lett. 2008 Oct 15; 18(20):5618-21.
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Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS. Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15; 18(22):5916-9.
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Koivunen JP, Mermel C, Zejnullahu K, Murphy C, Lifshits E, Holmes AJ, Choi HG, Kim J, Chiang D, Thomas R, Lee J, Richards WG, Sugarbaker DJ, Ducko C, Lindeman N, Marcoux JP, Engelman JA, Gray NS, Lee C, Meyerson M, Jänne PA. EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res. 2008 Jul 01; 14(13):4275-83.
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Plouffe D, Brinker A, McNamara C, Henson K, Kato N, Kuhen K, Nagle A, Adrián F, Matzen JT, Anderson P, Nam TG, Gray NS, Chatterjee A, Janes J, Yan SF, Trager R, Caldwell JS, Schultz PG, Zhou Y, Winzeler EA. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl Acad Sci U S A. 2008 Jul 01; 105(26):9059-64.
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Kato N, Sakata T, Breton G, Le Roch KG, Nagle A, Andersen C, Bursulaya B, Henson K, Johnson J, Kumar KA, Marr F, Mason D, McNamara C, Plouffe D, Ramachandran V, Spooner M, Tuntland T, Zhou Y, Peters EC, Chatterjee A, Schultz PG, Ward GE, Gray N, Harper J, Winzeler EA. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun; 4(6):347-56.
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McDermott U, Iafrate AJ, Gray NS, Shioda T, Classon M, Maheswaran S, Zhou W, Choi HG, Smith SL, Dowell L, Ulkus LE, Kuhlmann G, Greninger P, Christensen JG, Haber DA, Settleman J. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res. 2008 May 01; 68(9):3389-95.
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Goldstein DM, Gray NS, Zarrinkar PP. High-throughput kinase profiling as a platform for drug discovery. Nat Rev Drug Discov. 2008 May; 7(5):391-7.
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Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS. Discovery of selective aminothiazole aurora kinase inhibitors. ACS Chem Biol. 2008 Mar 20; 3(3):180-92.
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McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11; 104(50):19936-41.
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Jansma A, Zhang Q, Li B, Ding Q, Uno T, Bursulaya B, Liu Y, Furet P, Gray NS, Geierstanger BH. Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy. J Med Chem. 2007 Nov 29; 50(24):5875-7.
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Peters EC, Gray NS. Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. ACS Chem Biol. 2007 Oct 19; 2(10):661-4.
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Supekova L, Supek F, Lee J, Chen S, Gray N, Pezacki JP, Schlapbach A, Schultz PG. Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening. J Biol Chem. 2008 Jan 04; 283(1):29-36.
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2007

Hong J, Lee J, Min KH, Walker JR, Peters EC, Gray NS, Cho CY, Schultz PG. Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. ACS Chem Biol. 2007 Mar 20; 2(3):171-5.
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Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, Gray NS, Warmuth M. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 02; 104(1):270-5.
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2006

Gray NS. Drug discovery through industry-academic partnerships. Nat Chem Biol. 2006 Dec; 2(12):649-53.
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Pan S, Mi Y, Pally C, Beerli C, Chen A, Guerini D, Hinterding K, Nuesslein-Hildesheim B, Tuntland T, Lefebvre S, Liu Y, Gao W, Chu A, Brinkmann V, Bruns C, Streiff M, Cannet C, Cooke N, Gray N. A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol. 2006 Nov; 13(11):1227-34.
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Liu Y, Gray NS. Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol. 2006 Jul; 2(7):358-64.
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Okram B, Nagle A, Adrián FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS. A general strategy for creating “inactive-conformation” abl inhibitors. Chem Biol. 2006 Jul; 13(7):779-86.
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Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Che J, Lee CC, Caldwell J, Kanazawa T, Umemura I, Matsuura N, Ohmori O, Honda T, Gray N, He Y. Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorg Med Chem Lett. 2006 May 15; 16(10):2689-92.
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Nagle A, Hur W, Gray NS. Antimitotic agents of natural origin. Curr Drug Targets. 2006 Mar; 7(3):305-26.
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Zhang Q, Liu Y, Gao F, Ding Q, Cho C, Hur W, Jin Y, Uno T, Joazeiro CA, Gray N. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J Am Chem Soc. 2006 Feb 22; 128(7):2182-3.
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Melnick JS, Janes J, Kim S, Chang JY, Sipes DG, Gunderson D, Jarnes L, Matzen JT, Garcia ME, Hood TL, Beigi R, Xia G, Harig RA, Asatryan H, Yan SF, Zhou Y, Gu XJ, Saadat A, Zhou V, King FJ, Shaw CM, Su AI, Downs R, Gray NS, Schultz PG, Warmuth M, Caldwell JS. An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A. 2006 Feb 28; 103(9):3153-8.
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Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Sim T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Ohmori O, Caldwell J, Gray N, He Y. Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. Bioorg Med Chem Lett. 2006 Apr 15; 16(8):2173-6.
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Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P, Mestan J, Fabbro D, Gray NS. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb; 2(2):95-102.
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2005

Han S, Zhou V, Pan S, Liu Y, Hornsby M, McMullan D, Klock HE, Haugen J, Lesley SA, Gray N, Caldwell J, Gu XJ. Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005 Dec 15; 15(24):5467-73.
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Tang L, Li MH, Cao P, Wang F, Chang WR, Bach S, Reinhardt J, Ferandin Y, Galons H, Wan Y, Gray N, Meijer L, Jiang T, Liang DC. Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. J Biol Chem. 2005 Sep 02; 280(35):31220-9.
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Bach S, Knockaert M, Reinhardt J, Lozach O, Schmitt S, Baratte B, Koken M, Coburn SP, Tang L, Jiang T, Liang DC, Galons H, Dierick JF, Pinna LA, Meggio F, Totzke F, Schächtele C, Lerman AS, Carnero A, Wan Y, Gray N, Meijer L. Roscovitine targets, protein kinases and pyridoxal kinase. J Biol Chem. 2005 Sep 02; 280(35):31208-19.
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Luesch H, Wu TY, Ren P, Gray NS, Schultz PG, Supek F. A genome-wide overexpression screen in yeast for small-molecule target identification. Chem Biol. 2005 Jan; 12(1):55-63.
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2004

Li B, Liu Y, Uno T, Gray N. Creating chemical diversity to target protein kinases. Comb Chem High Throughput Screen. 2004 Aug; 7(5):453-72.
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Wu X, Ding S, Ding Q, Gray NS, Schultz PG. Small molecules that induce cardiomyogenesis in embryonic stem cells. J Am Chem Soc. 2004 Feb 18; 126(6):1590-1.
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Wan Y, Hur W, Cho CY, Liu Y, Adrian FJ, Lozach O, Bach S, Mayer T, Fabbro D, Meijer L, Gray NS. Synthesis and target identification of hymenialdisine analogs. Chem Biol. 2004 Feb; 11(2):247-59.
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Sanna MG, Liao J, Jo E, Alfonso C, Ahn MY, Peterson MS, Webb B, Lefebvre S, Chun J, Gray N, Rosen H. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem. 2004 Apr 02; 279(14):13839-48.
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Wignall SM, Gray NS, Chang YT, Juarez L, Jacob R, Burlingame A, Schultz PG, Heald R. Identification of a novel protein regulating microtubule stability through a chemical approach. Chem Biol. 2004 Jan; 11(1):135-46.
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2003

Ding S, Wu TY, Brinker A, Peters EC, Hur W, Gray NS, Schultz PG. Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci U S A. 2003 Jun 24; 100(13):7632-7.
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Chao SH, Walker JR, Chanda SK, Gray NS, Caldwell JS. Identification of homeodomain proteins, PBX1 and PREP1, involved in the transcription of murine leukemia virus. Mol Cell Biol. 2003 Feb; 23(3):831-41.
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Warmuth M, Damoiseaux R, Liu Y, Fabbro D, Gray N. SRC family kinases: potential targets for the treatment of human cancer and leukemia. Curr Pharm Des. 2003; 9(25):2043-59.
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Gray NS. Optimization of experimental antimitotic agents: classical and combinatorial methods. Prog Cell Cycle Res. 2003; 5:135-43.
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Ruetz S, Fabbro D, Zimmermann J, Meyer T, Gray N. Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. Curr Med Chem Anticancer Agents. 2003 Jan; 3(1):1-14.
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2002

Wu X, Ding S, Ding Q, Gray NS, Schultz PG. A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. J Am Chem Soc. 2002 Dec 11; 124(49):14520-1.
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Knockaert M, Lenormand P, Gray N, Schultz P, Pouysségur J, Meijer L. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 2002 Sep 19; 21(42):6413-24.
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Chang YT, Choi G, Bae YS, Burdett M, Moon HS, Lee JW, Gray NS, Schultz PG, Meijer L, Chung SK, Choi KY, Suh PG, Ryu SH. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem. 2002 Sep 02; 3(9):897-901.
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Schang LM, Bantly A, Knockaert M, Shaheen F, Meijer L, Malim MH, Gray NS, Schaffer PA. Pharmacological cyclin-dependent kinase inhibitors inhibit replication of wild-type and drug-resistant strains of herpes simplex virus and human immunodeficiency virus type 1 by targeting cellular, not viral, proteins. J Virol. 2002 Aug; 76(15):7874-82.
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Ding S, Gray NS, Ding Q, Wu X, Schultz PG. Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. J Comb Chem. 2002 Mar-Apr; 4(2):183-6.
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Ding S, Gray NS, Wu X, Ding Q, Schultz PG. A combinatorial scaffold approach toward kinase-directed heterocycle libraries. J Am Chem Soc. 2002 Feb 27; 124(8):1594-6.
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2001

Chang YT, Wignall SM, Rosania GR, Gray NS, Hanson SR, Su AI, Merlie J, Moon HS, Sangankar SB, Perez O, Heald R, Schultz PG. Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. J Med Chem. 2001 Dec 20; 44(26):4497-500.
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Ding S, Gray NS, Ding Q, Schultz PG. A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines. J Org Chem. 2001 Nov 30; 66(24):8273-6.
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Ding S, Gray NS, Ding Q, Schultz PG. Expanding the diversity of purine libraries. Tetrahedron Lett 2001;42:8751-5

Wu TY, Ding S, Gray NS, Schultz PG. Solid-phase synthesis of 2,3,5-trisubstituted indoles. Org Lett. 2001 Nov 29; 3(24):3827-30.
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Lin Q, Jiang F, Schultz PG, Gray NS. Design of allele-specific protein methyltransferase inhibitors. J Am Chem Soc. 2001 Nov 28; 123(47):11608-13.
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Gray NS. Combinatorial libraries and biological discovery. Curr Opin Neurobiol. 2001 Oct; 11(5):608-14.
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Verdugo DE, Cancilla MT, Ge X, Gray NS, Chang YT, Schultz PG, Negishi M, Leary JA, Bertozzi CR. Discovery of estrogen sulfotransferase inhibitors from a purine library screen. J Med Chem. 2001 Aug 16; 44(17):2683-6.
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Harmse L, van Zyl R, Gray N, Schultz P, Leclerc S, Meijer L, Doerig C, Havlik I. Structure-activity relationships and inhibitory effects of various purine derivatives on the in vitro growth of Plasmodium falciparum. Biochem Pharmacol. 2001 Aug 01; 62(3):341-8.
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2000

Bishop AC, Ubersax JA, Petsch DT, Matheos DP, Gray NS, Blethrow J, Shimizu E, Tsien JZ, Schultz PG, Rose MD, Wood JL, Morgan DO, Shokat KM. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21; 407(6802):395-401.
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Armstrong JI, Portley AR, Chang YT, Nierengarten DM, Cook BN, Bowman KG, Bishop A, Gray NS, Shokat KM, Schultz PG, Bertozzi CR. Discovery of Carbohydrate Sulfotransferase Inhibitors from a Kinase-Directed Library. Angew Chem Int Ed Engl 2000;39:1303-6.

Knockaert M, Gray N, Damiens E, Chang YT, Grellier P, Grant K, Fergusson D, Mottram J, Soete M, Dubremetz JF, Le Roch K, Doerig C, Schultz P, Meijer L. Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors. Chem Biol. 2000 Jun; 7(6):411-22.
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1999

Gray N, Détivaud L, Doerig C, Meijer L. ATP-site directed inhibitors of cyclin-dependent kinases. Curr Med Chem. 1999 Sep; 6(9):859-75.
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Chang YT, Gray NS, Rosania GR, Sutherlin DP, Kwon S, Norman TC, Sarohia R, Leost M, Meijer L, Schultz PG. Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. Chem Biol. 1999 Jun; 6(6):361-75.
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Rosania GR, Merlie J, Gray N, Chang YT, Schultz PG, Heald R. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999 Apr 27; 96(9):4797-802.
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1998

Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24; 281(5376):533-8.
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1997

Brooks EE, Gray NS, Joly A, Kerwar SS, Lum R, Mackman RL, Norman TC, Rosete J, Rowe M, Schow SR, Schultz PG, Wang X, Wick MM, Shiffman D. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14; 272(46):29207-11.
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Gray NS, Kwon S, Schultz PG. Combinatorial synthesis of 2,9-substituted purines. Tetrahedron Lett. 1997; 38:1161-4.

1996

Norman TC, Gray NS, Koh JT, Schultz PG. A structure-based approach to kinase inhibitors. J Am Chem Soc 1996;118:7430-1.

Patten PA, Gray NS, Yang PL, Marks CB, Wedemayer GJ, Boniface JJ, Stevens RC, Schultz PG. The immunological evolution of catalysis. Science. 1996 Feb 23; 271(5252):1086-91.
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