Nathanael Gray - Publications

Harvard University, Cambridge, MA, United States 
Cell Biology, Organic Chemistry, Biochemistry

359 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2019 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 Medicinal Chemistry Letters. 10: 1549-1553. PMID 31749909 DOI: 10.1021/acsmedchemlett.9b00381  0.76
2019 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 Chemical Biology. PMID 31735695 DOI: 10.1016/j.chembiol.2019.10.013  0.84
2019 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. PMID 31697837 DOI: 10.1182/blood.2019001576  1
2019 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. Nature Chemical Biology. PMID 31686031 DOI: 10.1038/s41589-019-0378-3  0.72
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 Infectious Diseases. PMID 31675213 DOI: 10.1021/acsinfecdis.9b00401  1
2019 Zhang T, Hatcher JM, Teng M, Gray NS, Kostic M. Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. Cell Chemical Biology. PMID 31631011 DOI: 10.1016/j.chembiol.2019.09.012  0.84
2019 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, ... ... Gray NS, et al. A kinase-independent role for CDK8 in BCR-ABL1 leukemia. Nature Communications. 10: 4741. PMID 31628323 DOI: 10.1038/s41467-019-12656-x  1
2019 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 Medicinal Chemistry Letters. 10: 1443-1449. PMID 31620231 DOI: 10.1021/acsmedchemlett.9b00243  1
2019 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, ... ... Gray NS, et al. Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. Cell Reports. 29: 118-134.e8. PMID 31577942 DOI: 10.1016/j.celrep.2019.08.090  0.32
2019 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. PMID 31455850 DOI: 10.1038/s41375-019-0552-3  1
2019 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, et al. BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells. Nature. PMID 31391581 DOI: 10.1038/s41586-019-1472-0  0.64
2019 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. Nature Communications. 10: 3468. PMID 31371704 DOI: 10.1038/s41467-019-11429-w  0.88
2019 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 gene expression exerts therapeutic effects on human Rett syndrome neurons and mutant mice. Science Translational Medicine. 11. PMID 31366578 DOI: 10.1126/scitranslmed.aau0164  1
2019 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, et al. Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies. British Journal of Haematology. PMID 31309543 DOI: 10.1111/bjh.16092  1
2019 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. Bioorganic & Medicinal Chemistry Letters. PMID 31175010 DOI: 10.1016/j.bmcl.2019.05.024  1
2019 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. Bioorganic & Medicinal Chemistry Letters. PMID 31129051 DOI: 10.1016/j.bmcl.2019.05.040  0.84
2019 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, ... ... Gray NS, et al. Single and dual targeting of mutant EGFR with an allosteric inhibitor. Cancer Discovery. PMID 31092401 DOI: 10.1158/2159-8290.CD-18-0903  0.76
2019 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, ... ... Gray NS, et al. BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models. Cancer Cell. 35: 752-766.e9. PMID 31085176 DOI: 10.1016/j.ccell.2019.04.005  0.76
2019 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 tumorigenic properties of melanoma cells. Acs Chemical Biology. PMID 31063355 DOI: 10.1021/acschembio.9b00083  0.72
2019 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, et al. CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation. Nature Communications. 10: 1757. PMID 30988284 DOI: 10.1038/s41467-019-09703-y  0.8
2019 Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Li T, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, ... ... Gray NS, et al. Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chemical Biology. PMID 30982749 DOI: 10.1016/j.chembiol.2019.02.021  0.84
2019 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 Chemical Biology. PMID 30956147 DOI: 10.1016/j.chembiol.2019.02.018  1
2019 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. Bioorganic & Medicinal Chemistry Letters. PMID 30954428 DOI: 10.1016/j.bmcl.2019.03.046  0.84
2019 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 Chemical Biology. PMID 30930164 DOI: 10.1016/j.chembiol.2019.02.015  1
2019 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. 8. PMID 30907729 DOI: 10.7554/eLife.45457  1
2019 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, ... ... Gray NS, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chemical Biology. PMID 30905681 DOI: 10.1016/j.chembiol.2019.02.012  0.84
2019 Rao S, Du G, Hafner M, Subramanian K, Sorger PK, Gray NS. A multi-targeted probe-based strategy to identify signaling vulnerabilities in cancers. The Journal of Biological Chemistry. PMID 30858179 DOI: 10.1074/jbc.RA118.006805  0.68
2019 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. Angewandte Chemie (International Ed. in English). PMID 30802347 DOI: 10.1002/anie.201901336  0.8
2019 Sung Hsieh HH, 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, ... ... Gray N, et al. Coordinating Tissue Regeneration through TGF-β Activated Kinase 1 (TAK1) In-activation and Re-activation. Stem Cells (Dayton, Ohio). PMID 30786091 DOI: 10.1002/stem.2991  0.56
2019 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 Research. PMID 30771406 DOI: 10.1016/j.antiviral.2019.02.008  1
2019 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). The Journal of Biological Chemistry. PMID 30679311 DOI: 10.1074/jbc.RA118.005428  0.92
2019 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, ... ... Gray NS, et al. Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nature Medicine. PMID 30664779 DOI: 10.1038/s41591-018-0312-3  0.72
2019 Li PC, Jang J, Hsia CY, Groomes P, Lian W, de Wispelaere M, Pitts JD, Wang J, Kwaitkowski N, Gray NS, Yang PL. Small molecules targeting the flavivirus E protein with broad-spectrum activity and antiviral efficacy in vivo. Acs Infectious Diseases. PMID 30608640 DOI: 10.1021/acsinfecdis.8b00322  1
2018 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 Chemical Biology. PMID 30595531 DOI: 10.1016/j.chembiol.2018.11.006  0.8
2018 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's Tyrosine Kinase degradation as a therapeutic strategy for cancer. Blood. PMID 30545835 DOI: 10.1182/blood-2018-07-862953  0.68
2018 Browne CM, Jiang B, Ficarro SB, Doctor ZM, Johnson JL, Card JD, Sivakumaren SC, Alexander WM, Yaron T, 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. Journal of the American Chemical Society. PMID 30518210 DOI: 10.1021/jacs.8b07911  0.84
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, et al. Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife. 7. PMID 30431433 DOI: 10.7554/eLife.41305  0.56
2018 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, ... ... Gray NS, et al. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 7. PMID 30422115 DOI: 10.7554/eLife.39030  1
2018 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, et al. A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation. Nature Cell Biology. PMID 30397315 DOI: 10.1038/s41556-018-0221-1  0.56
2018 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. PMID 30245209 DOI: 10.1016/j.stemcr.2018.08.016  0.88
2018 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 MA, ... ... Gray NS, et al. A high-throughput immune-oncology screen identifies EGFR inhibitors as potent enhancers of antigen-specific cytotoxic T-lymphocyte tumor cell killing. Cancer Immunology Research. PMID 30242021 DOI: 10.1158/2326-6066.CIR-18-0193  0.48
2018 Cho H, Shin I, Joo 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. Journal of Medicinal Chemistry. PMID 30153003 DOI: 10.1021/acs.jmedchem.8b00882  0.96
2018 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, ... ... Gray NS, et al. Structural and atropisomeric factors governing the selectivity of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains. Acs Chemical Biology. PMID 30102854 DOI: 10.1021/acschembio.7b00638  1
2018 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. Journal of Medicinal Chemistry. PMID 30095246 DOI: 10.1021/acs.jmedchem.7b01847  1
2018 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 Infectious Diseases. PMID 30027735 DOI: 10.1021/acsinfecdis.8b00127  1
2018 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, ... ... Gray NS, et al. Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth. The Journal of Clinical Investigation. PMID 30024860 DOI: 10.1172/JCI99436  0.84
2018 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 Research. PMID 30012673 DOI: 10.1158/0008-5472.CAN-17-3615  0.84
2018 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. 174: 300-311.e11. PMID 30007416 DOI: 10.1016/j.cell.2018.06.026  0.88
2018 Chao LH, Jang J, Johnson A, Nguyen A, Gray N, Yang PL, Harrison SC. How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion. Elife. 7. PMID 29999491 DOI: 10.7554/eLife.36461  0.88
2018 Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq D, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS. Discovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor. Angewandte Chemie (International Ed. in English). PMID 29978938 DOI: 10.1002/anie.201805187  0.84
2018 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 Medicinal Chemistry Letters. 9: 540-545. PMID 29937979 DOI: 10.1021/acsmedchemlett.8b00011  0.84
2018 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, et al. Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein. Cell Chemical Biology. PMID 29937406 DOI: 10.1016/j.chembiol.2018.05.011  1
2018 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. Nature Chemical Biology. PMID 29892083 DOI: 10.1038/s41589-018-0055-y  0.72
2018 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 Chemical Biology. PMID 29763550 DOI: 10.1021/acschembio.8b00154  0.72
2018 Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Janne PA, George RE, Gray NS. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). Journal of Medicinal Chemistry. PMID 29660984 DOI: 10.1021/acs.jmedchem.7b01655  0.64
2018 Bockorny B, Rusan M, Chen W, Liao RG, Li Y, Piccioni F, Wang J, Tan L, Thorner AR, Li T, Zhang Y, Miao CH, Ovesen T, Shapiro GI, Kwiatkowski DJ, ... Gray NS, et al. RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade. Molecular Cancer Therapeutics. PMID 29654068 DOI: 10.1158/1535-7163.MCT-17-0464  1
2018 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, ... ... Gray NS, et al. The dTAG system for immediate and target-specific protein degradation. Nature Chemical Biology. PMID 29581585 DOI: 10.1038/s41589-018-0021-8  0.64
2018 Ferguson FM, Gray NS. Kinase inhibitors: the road ahead. Nature Reviews. Drug Discovery. PMID 29545548 DOI: 10.1038/nrd.2018.21  1
2018 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, et al. Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 7. PMID 29528283 DOI: 10.7554/eLife.36414  0.72
2018 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, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nature Chemical Biology. PMID 29507391 DOI: 10.1038/s41589-018-0010-y  0.76
2018 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. Proceedings of the National Academy of Sciences of the United States of America. PMID 29507229 DOI: 10.1073/pnas.1707929115  1
2018 Chen JG, Liu X, Munshi M, Xu L, Tsakmaklis N, Demos MG, Kofides A, Guerrera ML, Chan GG, Patterson CJ, Meid KE, Gustine J, Dubeau T, Severns P, Castillo JJ, ... ... Gray NS, et al. BTKdrives ibrutinib resistance via ERK1/2, and protects BTKMYD88 mutated cells by a paracrine mechanism. Blood. PMID 29496671 DOI: 10.1182/blood-2017-10-811752  1
2018 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. PMID 29483645 DOI: 10.1038/s41388-018-0164-9  1
2018 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, et al. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chemical Biology. PMID 29478907 DOI: 10.1016/j.chembiol.2018.01.013  0.84
2018 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, ... ... Gray N, et al. Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations. Cancer Cell. 33: 173-186.e5. PMID 29438694 DOI: 10.1016/j.ccell.2018.01.004  0.8
2018 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. The Journal of Investigative Dermatology. PMID 29408204 DOI: 10.1016/j.jid.2017.09.056  0.8
2018 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, ... ... Gray NS, et al. Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation. Nature Communications. 9: 476. PMID 29396402 DOI: 10.1038/s41467-017-02811-7  0.76
2018 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, et al. EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma. Cancer Cell. PMID 29358035 DOI: 10.1016/j.ccell.2017.12.009  0.8
2018 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, ... ... Gray NS, et al. The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations. Cell Systems. 6: 13-24. PMID 29199020 DOI: 10.1016/j.cels.2017.11.001  0.64
2017 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 Chemical Biology. PMID 29276047 DOI: 10.1016/j.chembiol.2017.11.007  0.84
2017 Terai H, Kitajima S, Potter DS, Matsui Y, Gutierrez Quiceno L, Chen T, Kim TJ, Rusan M, Thai TC, Piccioni F, Donovan KA, Kwiatkowski N, Hinohara K, Wei G, Gray NS, et al. ER stress signaling promotes the survival of cancer 'persister cells' tolerant to EGFR tyrosine kinase inhibitors. Cancer Research. PMID 29259014 DOI: 10.1158/0008-5472.CAN-17-1904  0.8
2017 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, ... ... Gray NS, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nature Chemical Biology. PMID 29251720 DOI: 10.1038/nchembio.2538  0.84
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, et al. YY1 Is a Structural Regulator of Enhancer-Promoter Loops. Cell. 171: 1573-1588.e28. PMID 29224777 DOI: 10.1016/j.cell.2017.11.008  0.56
2017 Wang L, Qiao Q, Ferrao R, Shen C, Hatcher JM, Buhrlage SJ, Gray NS, Wu H. Crystal structure of human IRAK1. Proceedings of the National Academy of Sciences of the United States of America. PMID 29208712 DOI: 10.1073/pnas.1714386114  0.92
2017 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, ... ... Gray NS, et al. A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles. Cell. 171: 1437-1452.e17. PMID 29195078 DOI: 10.1016/j.cell.2017.10.049  1
2017 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, ... ... Gray NS, et al. A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chemical Biology. PMID 29129717 DOI: 10.1016/j.chembiol.2017.10.005  0.88
2017 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, ... ... Gray NS, et al. CDK4/6 Inhibition Augments Anti-Tumor Immunity by Enhancing T Cell Activation. Cancer Discovery. PMID 29101163 DOI: 10.1158/2159-8290.CD-17-0915  0.6
2017 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, ... ... Gray NS, et al. Suppression of adaptive responses to targeted cancer therapy by transcriptional repression. Cancer Discovery. PMID 29054992 DOI: 10.1158/2159-8290.CD-17-0461  0.8
2017 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 Reports. 21: 467-481. PMID 29020632 DOI: 10.1016/j.celrep.2017.09.056  0.8
2017 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. PMID 28978570 DOI: 10.1182/blood-2017-06-792184  0.72
2017 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, ... ... Gray NS, et al. Inhibition of USP10 induces degradation of oncogenic FLT3. Nature Chemical Biology. PMID 28967922 DOI: 10.1038/nchembio.2486  0.88
2017 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, ... ... Gray NS, et al. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 6. PMID 28926338 DOI: 10.7554/eLife.26693  0.88
2017 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. Science Advances. 3: e1700898. PMID 28835924 DOI: 10.1126/sciadv.1700898  0.88
2017 Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS. Characterization of a highly selective inhibitor of the Aurora kinases. Bioorganic & Medicinal Chemistry Letters. PMID 28818446 DOI: 10.1016/j.bmcl.2017.08.016  1
2017 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, ... ... Gray NS, et al. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nature Chemical Biology. PMID 28805801 DOI: 10.1038/nchembio.2458  0.6
2017 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, ... ... Gray NS, et al. Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chemical Biology. PMID 28781124 DOI: 10.1016/j.chembiol.2017.06.017  0.84
2017 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 (London, England : 1993). PMID 28781083 DOI: 10.1016/j.str.2017.07.003  0.68
2017 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, et al. Progress towards a public chemogenomic set for protein kinases and a call for contributions. Plos One. 12: e0181585. PMID 28767711 DOI: 10.1371/journal.pone.0181585  0.76
2017 Wong KK, Liu Y, Li Y, Wang X, Liu F, Gao P, Quinn MM, Li F, Merlino AA, Benes CH, Liu Q, Gray NS. Gemcitabine and Chk1 inhibitor AZD7762 synergistically suppress the growth of Lkb1-deficient lung adenocarcinoma. Cancer Research. PMID 28754670 DOI: 10.1158/0008-5472.CAN-17-0567  1
2017 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. 12: e0181178. PMID 28727840 DOI: 10.1371/journal.pone.0181178  1
2017 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, ... ... Gray NS, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Molecular Cell. PMID 28673542 DOI: 10.1016/j.molcel.2017.06.004  0.6
2017 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, ... ... Gray NS, et al. Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. European Journal of Medicinal Chemistry. 137: 545-557. PMID 28628824 DOI: 10.1016/j.ejmech.2017.06.016  1
2017 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 Reports. 19: 2177-2184. PMID 28614705 DOI: 10.1016/j.celrep.2017.05.042  1
2017 Williams CAC, Gray NS, Findlay GM. A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening. Journal of Visualized Experiments : Jove. PMID 28570543 DOI: 10.3791/55515  0.4
2017 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, ... ... Gray NS, et al. Synergistic interactions with PI3K inhibition that induce apoptosis. Elife. 6. PMID 28561737 DOI: 10.7554/eLife.24523  1
2017 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. European Journal of Medicinal Chemistry. 136: 497-510. PMID 28528303 DOI: 10.1016/j.ejmech.2017.04.079  0.84
2017 Vollmer S, Strickson S, Zhang T, Gray N, Lee K, Rao V, Cohen P. The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-Like receptor agonists. The Biochemical Journal. PMID 28512203 DOI: 10.1042/BCJ20170097  0.72
2017 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, ... ... Gray N, et al. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Science Translational Medicine. 9. PMID 28490664 DOI: 10.1126/scitranslmed.aal2668  0.4
2017 Hatcher JM, Choi HG, Alessi DR, Gray NS. Small-Molecule Inhibitors of LRRK2. Advances in Neurobiology. 14: 241-264. PMID 28353288 DOI: 10.1007/978-3-319-49969-7_13  0.88
2017 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, ... ... Gray NS, et al. Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. Scientific Reports. 7: 466. PMID 28352114 DOI: 10.1038/s41598-017-00482-4  1
2017 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 Medicinal Chemistry Letters. 8: 344-349. PMID 28337328 DOI: 10.1021/acsmedchemlett.7b00008  1
2017 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, ... ... Gray NS, et al. Corrigendum: SIKs control osteocyte responses to parathyroid hormone. Nature Communications. 8: 14745. PMID 28224982 DOI: 10.1038/ncomms14745  1
2017 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, ... ... Gray NS, et al. Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nature Communications. 8: 14747. PMID 28218232 DOI: 10.1038/ncomms14747  0.8
2017 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, ... ... Gray NS, et al. THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nature Communications. 8: 14290. PMID 28134252 DOI: 10.1038/ncomms14290  0.8
2017 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 Medicinal Chemistry Letters. 8: 61-66. PMID 28105276 DOI: 10.1021/acsmedchemlett.6b00373  0.84
2017 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, ... ... Gray NS, et al. A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas. Neuro-Oncology. PMID 28082416 DOI: 10.1093/neuonc/now261  0.88
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. Analytical Chemistry. 88: 12248-12254. PMID 28193034 DOI: 10.1021/acs.analchem.6b03394  0.88
2016 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, et al. Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. Bioorganic & Medicinal Chemistry. PMID 28038940 DOI: 10.1016/j.bmc.2016.11.034  0.84
2016 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 Research. PMID 28034743 DOI: 10.1016/j.antiviral.2016.12.017  1
2016 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, et al. Structure-guided development of covalent TAK1 inhibitors. Bioorganic & Medicinal Chemistry. PMID 28011204 DOI: 10.1016/j.bmc.2016.11.035  0.84
2016 Beelontally R, Wilkie GS, Lau B, Goodmaker CJ, Ho CM, 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 Research. PMID 27956134 DOI: 10.1016/j.antiviral.2016.12.006  1
2016 Hur W, Rosen H, Gray NS. A benzo[b]thiophene-based selective type 4 S1P receptor agonist. Bioorganic & Medicinal Chemistry Letters. PMID 27894870 DOI: 10.1016/j.bmcl.2016.11.050  0.96
2016 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-δ/γ Inhibitors. Acs Medicinal Chemistry Letters. 7: 908-912. PMID 27774127 DOI: 10.1021/acsmedchemlett.6b00209  1
2016 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, ... ... Gray NS, et al. SIKs control osteocyte responses to parathyroid hormone. Nature Communications. 7: 13176. PMID 27759007 DOI: 10.1038/ncomms13176  0.52
2016 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, et al. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. PMID 27626175 DOI: 10.18632/oncotarget.11951  1
2016 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, ... ... Gray NS, et al. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nature Chemical Biology. PMID 27571479 DOI: 10.1038/nchembio.2166  0.64
2016 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, ... ... Gray NS, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Science Translational Medicine. 8: 352ra108. PMID 27535619 DOI: 10.1126/scitranslmed.aaf2304  0.88
2016 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. Proceedings of the National Academy of Sciences of the United States of America. PMID 27528663 DOI: 10.1073/pnas.1606862113  0.88
2016 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 Reports. PMID 27498864 DOI: 10.1016/j.celrep.2016.07.033  1
2016 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, ... ... Gray NS, et al. Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. Cancer Cell. PMID 27478041 DOI: 10.1016/j.ccell.2016.06.020  0.52
2016 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, ... ... Gray NS, et al. Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology. 12: 656. PMID 27434767 DOI: 10.1038/nchembio0816-656  0.92
2016 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, ... ... Gray NS, et al. A Landscape of Pharmacogenomic Interactions in Cancer. Cell. PMID 27397505 DOI: 10.1016/j.cell.2016.06.017  0.64
2016 Brown W, Tan L, Smith A, Gray NS, Wendt M. Covalent targeting of fibroblast growth factor receptor inhibits metastatic breast cancer. Molecular Cancer Therapeutics. PMID 27371729 DOI: 10.1158/1535-7163.MCT-16-0136  0.52
2016 Chong CR, Bahcall M, Capelletti M, Kosaka T, Ercan D, Sim T, Sholl LM, Nishino M, Johnson BE, Gray NS, Janne PA. Identification of existing drugs that effectively target NTRK1- and ROS1-rearrangements in lung cancer. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. PMID 27370605 DOI: 10.1158/1078-0432.CCR-15-1601  0.84
2016 Lee S, Shang Y, Redmond SA, Urisman A, Tang AA, Li KH, Burlingame AL, Pak RA, Jovičić A, Gitler AD, Wang J, Gray NS, Seeley WW, Siddique T, Bigio EH, et al. Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis. Neuron. PMID 27321923 DOI: 10.1016/j.neuron.2016.05.021  0.8
2016 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, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function In Vivo. Acs Chemical Biology. PMID 27224444 DOI: 10.1021/acschembio.6b00217  1
2016 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 Medicinal Chemistry Letters. 7: 476-81. PMID 27190596 DOI: 10.1021/acsmedchemlett.5b00498  1
2016 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, ... ... Gray NS, et al. Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. Blood. PMID 27151888 DOI: 10.1182/blood-2016-02-696856  0.88
2016 Yang G, Buhrlage S, 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, ... ... Gray N, et al. HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. Blood. PMID 27143257 DOI: 10.1182/blood-2016-01-695098  0.92
2016 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. Radiation Research. PMID 27135971 DOI: 10.1667/RR14373.1  0.8
2016 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, ... ... Gray NS, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology. PMID 27110680 DOI: 10.1038/nchembio.2070  0.6
2016 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 Chemical Biology. 23: 443-452. PMID 27105280 DOI: 10.1016/j.chembiol.2016.03.010  0.64
2016 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 YF, Wang L, Gray NS, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. Acs Chemical Biology. PMID 27082499 DOI: 10.1021/acschembio.6b00250  1
2016 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. British Journal of Haematology. PMID 27073043 DOI: 10.1111/bjh.14103  0.52
2016 Westover KD, Jänne PA, Gray NS. Progress on Covalent Inhibition of KRASG12C. Cancer Discovery. 6: 233-4. PMID 26951837 DOI: 10.1158/2159-8290.CD-16-0092  0.84
2016 Ho CM, Donovan-Banfield IZ, Tan L, Zhang T, Gray NS, Strang BL. Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells. Plos One. 11: e0150339. PMID 26930276 DOI: 10.1371/journal.pone.0150339  0.64
2016 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, et al. Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature. PMID 26886795 DOI: 10.1038/nature16963  0.8
2016 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 Research. PMID 26744526 DOI: 10.1158/0008-5472.CAN-15-0717  0.8
2015 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. The Journal of Investigative Dermatology. PMID 26739095 DOI: 10.1016/j.jid.2015.12.023  1
2015 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, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Research. PMID 26677978 DOI: 10.1158/0008-5472.CAN-15-0817  0.8
2015 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 (Pgp) function. British Journal of Pharmacology. PMID 26603906 DOI: 10.1111/bph.13395  0.8
2015 Hatcher JM, Bahcall M, Choi HG, Gao Y, Sim T, George R, Janne PA, Gray NS. Discovery of inhibitors that overcome the G1202R ALK resistance mutation. Journal of Medicinal Chemistry. PMID 26568289 DOI: 10.1021/acs.jmedchem.5b01136  1
2015 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, ... ... Gray N, et al. Corrigendum: The promise and peril of chemical probes. Nature Chemical Biology. 11: 887. PMID 26485080 DOI: 10.1038/nchembio1115-887c  0.76
2015 Müller S, Chaikuad A, Gray NS, Knapp S. The ins and outs of selective kinase inhibitor development. Nature Chemical Biology. 11: 818-21. PMID 26485069 DOI: 10.1038/nchembio.1938  1
2015 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. Molecular Cell. PMID 26439301 DOI: 10.1016/j.molcel.2015.09.001  0.64
2015 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, et al. CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer. Cell. 163: 174-186. PMID 26406377 DOI: 10.1016/j.cell.2015.08.063  1
2015 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 Chemical Biology. PMID 26390252 DOI: 10.1021/acschembio.5b00655  1
2015 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, ... ... Gray NS, et al. Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. Oncotarget. PMID 26375053  1
2015 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. Science Signaling. 8: ra86. PMID 26307013 DOI: 10.1126/scisignal.aaa3206  0.8
2015 Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella KM, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, ... ... Gray NS, et al. Development of Selective Covalent JAK3 Inhibitors. Journal of Medicinal Chemistry. PMID 26258521 DOI: 10.1021/acs.jmedchem.5b00710  1
2015 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, ... ... Gray N, et al. The promise and peril of chemical probes. Nature Chemical Biology. 11: 536-41. PMID 26196764 DOI: 10.1038/nchembio.1867  1
2015 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, ... ... Gray NS, et al. Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. Leukemia. PMID 26165234 DOI: 10.1038/leu.2015.180  0.8
2015 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. Bioorganic & Medicinal Chemistry Letters. 25: 3382-9. PMID 26094118 DOI: 10.1016/j.bmcl.2015.04.103  1
2015 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. 10: e0128364. PMID 26046350 DOI: 10.1371/journal.pone.0128364  1
2015 Tricker EM, Xu C, Uddin S, Capelletti M, Ercan D, Ogino A, Pratilas CA, Rosen N, Gray NS, Wong KK, Janne PA. Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR mutant Lung Cancer. Cancer Discovery. PMID 26036643 DOI: 10.1158/2159-8290.CD-15-0063  0.8
2015 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 Medicinal Chemistry Letters. 6: 584-9. PMID 26005538 DOI: 10.1021/acsmedchemlett.5b00064  1
2015 Wang J, Gray NS. SnapShot: Kinase Inhibitors II. Molecular Cell. 58: 710.e1. PMID 26000855 DOI: 10.1016/j.molcel.2015.05.002  1
2015 Wang J, Gray NS. SnapShot: Kinase Inhibitors I. Molecular Cell. 58: 708.e1. PMID 26000854 DOI: 10.1016/j.molcel.2015.05.001  1
2015 Ercan D, Choi HG, Yun CH, Capelletti M, Xie T, Eck MJ, Gray NS, Janne PA. EGFR mutations and resistance to Irreversible pyrimidine based EGFR inhibitors. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. PMID 25948633 DOI: 10.1158/1078-0432.CCR-14-2789  1
2015 Malik N, Vollmer S, Nanda SK, Lopez-Pelaez M, Prescott A, Gray N, Cohen P. Suppression of Interferon β gene transcription by inhibitors of Bromodomain and Extra-Terminal (BET) family members. The Biochemical Journal. PMID 25891802 DOI: 10.1042/BJ20141523  0.8
2015 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. 125: 3133-43. PMID 25833960 DOI: 10.1182/blood-2014-12-615906  0.92
2015 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. Molecular Systems Biology. 11: 797. PMID 25814555  0.72
2015 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 Discovery. 5: 274-87. PMID 25542448 DOI: 10.1158/2159-8290.CD-14-0295  1
2015 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. Chemical Biology & Drug Design. 86: 144-55. PMID 25376742 DOI: 10.1111/cbdd.12473  0.8
2015 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 Chemical Biology. 10: 299-309. PMID 25317566 DOI: 10.1021/cb500674s  0.8
2015 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. Molecular Oncology. 9: 260-9. PMID 25226813 DOI: 10.1016/j.molonc.2014.08.011  0.84
2015 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. 64: 1454-65. PMID 25183205 DOI: 10.1136/gutjnl-2014-306761  0.88
2015 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, ... ... Gray NS, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). Journal of Medicinal Chemistry. 58: 183-96. PMID 25075558 DOI: 10.1021/jm500480k  1
2015 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. 34: 2167-77. PMID 24909170 DOI: 10.1038/onc.2014.161  1
2015 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. 29: 27-37. PMID 24791855 DOI: 10.1038/leu.2014.149  1
2014 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, ... ... Gray NS, et al. Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 15: 524-526. PMID 28903030 DOI: 10.1016/j.stem.2014.09.003  0.88
2014 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, ... ... Gray NS, et al. Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 15: 523. PMID 28903029 DOI: 10.1016/j.stem.2014.08.002  0.88
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, ... ... Gray NS, et al. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 26: 909-22. PMID 25490451 DOI: 10.1016/j.ccell.2014.10.019  1
2014 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, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 159: 1126-39. PMID 25416950 DOI: 10.1016/j.cell.2014.10.024  1
2014 Gray NS, Fabbro D. Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. Methods in Enzymology. 548: 173-88. PMID 25399646 DOI: 10.1016/B978-0-12-397918-6.00007-0  0.36
2014 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. Science Signaling. 7: ra102. PMID 25351247 DOI: 10.1126/scisignal.2005470  0.88
2014 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, ... ... Gray NS, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proceedings of the National Academy of Sciences of the United States of America. 111: E4869-77. PMID 25349422 DOI: 10.1073/pnas.1403438111  1
2014 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. Nature Chemical Biology. 10: 1006-12. PMID 25326665 DOI: 10.1038/nchembio.1658  1
2014 Lopez-Pelaez M, Lamont DJ, Peggie M, Shpiro N, Gray NS, Cohen P. Protein kinase IKKβ-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells. Proceedings of the National Academy of Sciences of the United States of America. 111: 17432-7. PMID 25326418 DOI: 10.1073/pnas.1418399111  0.32
2014 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, et al. Response and acquired resistance to everolimus in anaplastic thyroid cancer. The New England Journal of Medicine. 371: 1426-33. PMID 25295501 DOI: 10.1056/NEJMoa1403352  0.92
2014 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. 14: 681. PMID 25236161 DOI: 10.1186/1471-2407-14-681  1
2014 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. 5: 8737-49. PMID 25228590  1
2014 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. Nature Chemical Biology. 10: 853-60. PMID 25195011 DOI: 10.1038/nchembio.1629  1
2014 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. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 20: 5483-95. PMID 25186968 DOI: 10.1158/1078-0432.CCR-14-0902  0.92
2014 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. Nature Communications. 5: 4763. PMID 25159004 DOI: 10.1038/ncomms5763  0.52
2014 Sundberg TB, Choi HG, Song JH, Russell CN, Hussain MM, Graham DB, Khor B, Gagnon J, O'Connell DJ, Narayan K, Dan?ík V, Perez JR, Reinecker HC, Gray NS, Schreiber SL, et al. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proceedings of the National Academy of Sciences of the United States of America. 111: 12468-73. PMID 25114223 DOI: 10.1073/pnas.1412308111  1
2014 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 : a European Journal of Chemical Biology. 15: 1920-30. PMID 25111632 DOI: 10.1002/cbic.201400025  1
2014 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, ... ... Gray NS, et al. Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell. 15: 471-87. PMID 25090446 DOI: 10.1016/j.stem.2014.07.002  0.64
2014 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, et al. The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nature Communications. 5: 4535. PMID 25088745 DOI: 10.1038/ncomms5535  1
2014 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, ... ... Gray NS, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 511: 616-20. PMID 25043025 DOI: 10.1038/nature13393  1
2014 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. Proceedings of the National Academy of Sciences of the United States of America. 111: 8895-900. PMID 24889603 DOI: 10.1073/pnas.1404639111  1
2014 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, et al. MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 3: e01763. PMID 24844244 DOI: 10.7554/eLife.01763  1
2014 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 : a European Journal of Chemical Biology. 15: 1317-24. PMID 24828915 DOI: 10.1002/cbic.201402010  1
2014 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. Journal of Molecular Biology. 426: 2457-70. PMID 24768818 DOI: 10.1016/j.jmb.2014.04.014  0.76
2014 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 Chemical Biology. 9: 1230-41. PMID 24730530 DOI: 10.1021/cb500129t  1
2014 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. The Journal of Clinical Investigation. 124: 2037-49. PMID 24713656 DOI: 10.1172/JCI72522  1
2014 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. 9: e92649. PMID 24667246 DOI: 10.1371/journal.pone.0092649  1
2014 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, et al. PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1). Molecular Cancer Therapeutics. 13: 1231-45. PMID 24659821 DOI: 10.1158/1535-7163.MCT-13-0575-T  1
2014 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, ... ... Gray NS, et al. Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma. Acs Chemical Biology. 9: 1086-91. PMID 24556163 DOI: 10.1021/cb4008524  1
2014 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. Journal of the American Society For Mass Spectrometry. 25: 636-50. PMID 24496597 DOI: 10.1007/s13361-013-0811-x  1
2014 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. Molecular Cancer Therapeutics. 13: 475-82. PMID 24296828 DOI: 10.1158/1535-7163.MCT-13-0817  1
2014 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, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angewandte Chemie (International Ed. in English). 53: 199-204. PMID 24259466 DOI: 10.1002/anie.201307387  1
2014 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. The Biochemical Journal. 457: 215-25. PMID 24171924 DOI: 10.1042/BJ20131152  1
2013 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, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. Acs Medicinal Chemistry Letters. 4: 333-7. PMID 24900670 DOI: 10.1021/ml300396r  1
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, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. European Journal of Medicinal Chemistry. 70: 758-67. PMID 24239623 DOI: 10.1016/j.ejmech.2013.10.052  1
2013 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. Molecular Cancer Therapeutics. 12: 2651-62. PMID 24130053 DOI: 10.1158/1535-7163.MCT-13-0103-T  1
2013 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, ... ... Gray NS, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. Journal of the National Cancer Institute. 105: 1322-31. PMID 23940287 DOI: 10.1093/jnci/djt168  1
2013 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, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. Acs Chemical Biology. 8: 2145-50. PMID 23899692 DOI: 10.1021/cb400430t  1
2013 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 (New York, N.Y.). 341: 1236566. PMID 23888043 DOI: 10.1126/science.1236566  1
2013 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. 122: 1222-32. PMID 23836557 DOI: 10.1182/blood-2012-12-475111  1
2013 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. Nature Biotechnology. 31: 630-7. PMID 23811600 DOI: 10.1038/nbt.2620  1
2013 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, et al. Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. Cancer Research. 73: 5195-205. PMID 23786770 DOI: 10.1158/0008-5472.CAN-12-3950  1
2013 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, ... ... Gray NS, et al. 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. Journal of Medicinal Chemistry. 56: 5675-90. PMID 23742252 DOI: 10.1021/jm400402q  1
2013 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, ... ... Gray NS, et al. Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. Cancer Discovery. 3: 870-9. PMID 23715154 DOI: 10.1158/2159-8290.CD-13-0015  1
2013 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. Journal of Medicinal Chemistry. 56: 4413-21. PMID 23656407 DOI: 10.1021/jm4000837  1
2013 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, ... ... Gray NS, et al. Discovery of a selective irreversible BMX inhibitor for prostate cancer. Acs Chemical Biology. 8: 1423-8. PMID 23594111 DOI: 10.1021/cb4000629  1
2013 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. 56: 1350-5. PMID 23475368 DOI: 10.1007/s00125-013-2877-1  1
2013 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, ... ... Gray NS, et al. TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discovery. 3: 564-77. PMID 23471820 DOI: 10.1158/2159-8290.CD-12-0504  1
2013 Liu Q, Sabnis Y, Zhao Z, Zhang T, Buhrlage SJ, Jones LH, Gray NS. Developing irreversible inhibitors of the protein kinase cysteinome. Chemistry & Biology. 20: 146-59. PMID 23438744 DOI: 10.1016/j.chembiol.2012.12.006  1
2013 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. 8: e56473. PMID 23437141 DOI: 10.1371/journal.pone.0056473  1
2013 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, ... ... Gray NS, et al. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Research. 73: 2574-86. PMID 23436801 DOI: 10.1158/0008-5472.CAN-12-1702  1
2013 Guo Y, Chekaluk Y, Zhang J, Du J, Gray NS, Wu CL, Kwiatkowski DJ. TSC1 involvement in bladder cancer: diverse effects and therapeutic implications. The Journal of Pathology. 230: 17-27. PMID 23401075 DOI: 10.1002/path.4176  0.88
2013 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, et al. A public-private partnership to unlock the untargeted kinome. Nature Chemical Biology. 9: 3-6. PMID 23238671 DOI: 10.1038/nchembio.1113  1
2013 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 Research. 73: 834-43. PMID 23172312 DOI: 10.1158/0008-5472.CAN-12-2066  1
2013 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. 32: 3156-64. PMID 22869143 DOI: 10.1038/onc.2012.332  1
2012 Koliwad SK, Gray NE, Wang JC. Angiopoietin-like 4 (Angptl4): A glucocorticoid-dependent gatekeeper of fatty acid flux during fasting. Adipocyte. 1: 182-187. PMID 23700531 DOI: 10.4161/adip.20787  0.72
2012 Deng X, Choi HG, Buhrlage SJ, Gray NS. Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011). Expert Opinion On Therapeutic Patents. 22: 1415-26. PMID 23126385 DOI: 10.1517/13543776.2012.729041  1
2012 Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. Acs Medicinal Chemistry Letters. 3: 658-662. PMID 23066449 DOI: 10.1021/ml300123a  1
2012 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. Proceedings of the National Academy of Sciences of the United States of America. 109: 16986-91. PMID 23033494 DOI: 10.1073/pnas.1215450109  1
2012 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, ... ... Gray NS, et al. Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discovery. 2: 934-47. PMID 22961667 DOI: 10.1158/2159-8290.CD-12-0103  1
2012 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. Bioorganic & Medicinal Chemistry Letters. 22: 5625-9. PMID 22863203 DOI: 10.1016/j.bmcl.2012.06.104  1
2012 Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS. Development of 'DFG-out' inhibitors of gatekeeper mutant kinases. Bioorganic & Medicinal Chemistry Letters. 22: 5297-302. PMID 22819762 DOI: 10.1016/j.bmcl.2012.06.036  0.88
2012 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. 7: e41343. PMID 22815993 DOI: 10.1371/journal.pone.0041343  0.72
2012 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. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 18: 4580-8. PMID 22791884 DOI: 10.1158/1078-0432.CCR-12-1157  1
2012 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, ... ... Gray NS, et al. The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell. 22: 117-30. PMID 22789543 DOI: 10.1016/j.ccr.2012.06.001  1
2012 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, PDGFRα and kit. Bioorganic & Medicinal Chemistry Letters. 22: 4579-84. PMID 22727638 DOI: 10.1016/j.bmcl.2012.05.107  1
2012 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. 7: e39132. PMID 22723946 DOI: 10.1371/journal.pone.0039132  1
2012 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. Molecular Biosystems. 8: 2523-6. PMID 22673640 DOI: 10.1039/c2mb25099c  1
2012 Wang JC, Gray NE, Kuo T, Harris CA. Regulation of triglyceride metabolism by glucocorticoid receptor. Cell & Bioscience. 2: 19. PMID 22640645 DOI: 10.1186/2045-3701-2-19  0.72
2012 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-p110β as a potential anticancer agent. Cancer Discovery. 2: 425-33. PMID 22588880 DOI: 10.1158/2159-8290.CD-12-0003  1
2012 Thoreen CC, Chantranupong L, Keys HR, Wang T, Gray NS, Sabatini DM. A unifying model for mTORC1-mediated regulation of mRNA translation. Nature. 485: 109-13. PMID 22552098 DOI: 10.1038/nature11083  1
2012 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. Chemistry & Biology. 19: 529-40. PMID 22520759 DOI: 10.1016/j.chembiol.2012.01.020  1
2012 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 Chemical Biology. 7: 982-7. PMID 22496512 DOI: 10.1021/cb300058v  1
2012 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, ... ... Gray N, et al. 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. 26: 2233-44. PMID 22469781 DOI: 10.1038/leu.2012.96  0.96
2012 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, ... ... Gray NS, et al. Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature. 483: 570-5. PMID 22460902 DOI: 10.1038/nature11005  1
2012 Zhang J, Deng X, Choi HG, Alessi DR, Gray NS. Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 22: 1864-9. PMID 22335897 DOI: 10.1016/j.bmcl.2012.01.084  1
2012 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, ... ... Gray NS, et al. Discovery of potent and selective covalent inhibitors of JNK. Chemistry & Biology. 19: 140-54. PMID 22284361 DOI: 10.1016/j.chembiol.2011.11.010  1
2012 Gray NE, Lam LN, Yang K, Zhou AY, Koliwad S, Wang JC. Angiopoietin-like 4 (Angptl4) protein is a physiological mediator of intracellular lipolysis in murine adipocytes. The Journal of Biological Chemistry. 287: 8444-56. PMID 22267746 DOI: 10.1074/jbc.M111.294124  0.72
2012 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, ... ... Gray NS, et al. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. The Journal of Biological Chemistry. 287: 9742-52. PMID 22223645 DOI: 10.1074/jbc.M111.304485  1
2012 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 in Molecular Biology (Clifton, N.J.). 821: 447-60. PMID 22125084 DOI: 10.1007/978-1-61779-430-8_29  1
2012 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 Chemical Biology. 7: 185-96. PMID 21992004 DOI: 10.1021/cb200305u  1
2011 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, ... ... Gray NS, et al. Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discovery. 1: 78-89. PMID 22328973 DOI: 10.1158/2159-8274.CD-11-0005  1
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, et al. Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nature Medicine. 17: 1116-20. PMID 21822287 DOI: 10.1038/nm.2402  1
2011 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. Chemistry & Biology. 18: 868-79. PMID 21802008 DOI: 10.1016/j.chembiol.2011.05.010  1
2011 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, ... ... Gray NS, et al. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Research. 71: 6051-60. PMID 21791641 DOI: 10.1158/0008-5472.CAN-11-1340  1
2011 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. 6: e20226. PMID 21750699 DOI: 10.1371/journal.pone.0020226  1
2011 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, et al. In situ kinase profiling reveals functionally relevant properties of native kinases. Chemistry & Biology. 18: 699-710. PMID 21700206 DOI: 10.1016/j.chembiol.2011.04.011  1
2011 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. 6: e20351. PMID 21666749 DOI: 10.1371/journal.pone.0020351  1
2011 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 (New York, N.Y.). 332: 1317-22. PMID 21659604 DOI: 10.1126/science.1199498  1
2011 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. Bioorganic & Medicinal Chemistry Letters. 21: 4036-40. PMID 21621413 DOI: 10.1016/j.bmcl.2011.04.129  1
2011 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 Medicinal Chemistry Letters. 2: 379-384. PMID 21572589 DOI: 10.1021/ml200002a  1
2011 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 Medicinal Chemistry Letters. 2: 195-200. PMID 21412406 DOI: 10.1021/ml100304b  0.88
2011 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. Nature Chemical Biology. 7: 203-5. PMID 21378983 DOI: 10.1038/nchembio.538  1
2011 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. Journal of Medicinal Chemistry. 54: 1473-80. PMID 21322566 DOI: 10.1021/jm101520v  1
2011 Iacob RE, Zhang J, Gray NS, Engen JR. Allosteric interactions between the myristate- and ATP-site of the Abl kinase. Plos One. 6: e15929. PMID 21264348 DOI: 10.1371/journal.pone.0015929  1
2011 Zhou W, Ercan D, Jänne PA, Gray NS. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorganic & Medicinal Chemistry Letters. 21: 638-43. PMID 21208802 DOI: 10.1016/j.bmcl.2010.12.036  0.88
2011 Hur W, Gray NS. Small molecule modulators of antioxidant response pathway. Current Opinion in Chemical Biology. 15: 162-73. PMID 21195017 DOI: 10.1016/j.cbpa.2010.12.009  0.96
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 Research. 70: 10038-43. PMID 21030459 DOI: 10.1158/0008-5472.CAN-10-2956  1
2010 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, ... ... Gray NS, et al. Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Research. 70: 9827-36. PMID 20952506 DOI: 10.1158/0008-5472.CAN-10-1671  1
2010 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. Journal of Medicinal Chemistry. 53: 7146-55. PMID 20860370 DOI: 10.1021/jm101144f  1
2010 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. 18: 258-67. PMID 20832753 DOI: 10.1016/j.ccr.2010.08.008  1
2010 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. Journal of Medicinal Chemistry. 53: 6934-46. PMID 20828158 DOI: 10.1021/jm100555f  1
2010 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, et al. Discovery and characterization of novel mutant FLT3 kinase inhibitors. Molecular Cancer Therapeutics. 9: 2468-77. PMID 20807780 DOI: 10.1158/1535-7163.MCT-10-0232  0.88
2010 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, ... ... Gray NS, et al. Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. Bioorganic & Medicinal Chemistry Letters. 20: 4027-31. PMID 20610151 DOI: 10.1016/j.bmcl.2010.05.095  0.96
2010 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, et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. Journal of Medicinal Chemistry. 53: 5439-48. PMID 20604564 DOI: 10.1021/jm901808w  1
2010 Deng X, Lim SM, Zhang J, Gray NS. Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorganic & Medicinal Chemistry Letters. 20: 4196-200. PMID 20541934 DOI: 10.1016/j.bmcl.2010.05.043  0.88
2010 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. Chemistry & Biology. 17: 537-47. PMID 20534351 DOI: 10.1016/j.chembiol.2010.03.013  1
2010 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. 24: 1375-8. PMID 20508612 DOI: 10.1038/leu.2010.107  0.88
2010 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. Nature Chemical Biology. 6: 359-68. PMID 20383151 DOI: 10.1038/nchembio.345  1
2010 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. Chemistry & Biology. 17: 285-95. PMID 20338520 DOI: 10.1016/j.chembiol.2010.02.007  1
2010 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, ... ... Gray N, et al. 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. 115: 4206-16. PMID 20299508 DOI: 10.1182/blood-2009-11-251751  0.88
2010 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, et al. Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochimica Et Biophysica Acta. 1804: 454-62. PMID 20152788 DOI: 10.1016/j.bbapap.2009.12.009  0.88
2010 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 Research. 70: 1625-34. PMID 20124471 DOI: 10.1158/0008-5472.CAN-09-3620  1
2010 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, ... ... Gray NS, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 463: 501-6. PMID 20072125 DOI: 10.1038/nature08675  1
2009 Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today. Therapeutic Strategies. 6: 47-55. PMID 20622997 DOI: 10.1016/j.ddstr.2009.12.001  1
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. 462: 1070-4. PMID 20033049 DOI: 10.1038/nature08622  1
2009 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, et al. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proceedings of the National Academy of Sciences of the United States of America. 106: 20411-6. PMID 19915144 DOI: 10.1073/pnas.0905833106  1
2009 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, ... ... Gray NS, et al. Cell-based optimization of novel benzamides as potential antimalarial leads. Bioorganic & Medicinal Chemistry Letters. 19: 6970-4. PMID 19879133 DOI: 10.1016/j.bmcl.2009.10.050  0.96
2009 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, et al. Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorganic & Medicinal Chemistry Letters. 19: 6691-5. PMID 19854052 DOI: 10.1016/j.bmcl.2009.09.123  1
2009 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. The Journal of Biological Chemistry. 284: 29005-14. PMID 19679652 DOI: 10.1074/jbc.M109.026633  1
2009 Jänne PA, Gray N, Settleman J. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nature Reviews. Drug Discovery. 8: 709-23. PMID 19629074 DOI: 10.1038/nrd2871  0.52
2009 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. Bioorganic & Medicinal Chemistry Letters. 19: 4467-70. PMID 19553108 DOI: 10.1016/j.bmcl.2009.05.029  1
2009 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 Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy. 12: 81-9. PMID 19467916 DOI: 10.1016/j.drup.2009.04.001  0.92
2009 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. 137: 873-86. PMID 19446321 DOI: 10.1016/j.cell.2009.03.046  1
2009 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 Research. 69: 2244-51. PMID 19258500 DOI: 10.1158/0008-5472.CAN-08-3398  1
2009 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. Immunology Letters. 123: 1-8. PMID 19185589 DOI: 10.1016/j.imlet.2008.12.011  0.56
2009 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. Nature Chemical Biology. 5: 157-65. PMID 19182783 DOI: 10.1038/nchembio.144  0.76
2009 Iacob RE, Pene-Dumitrescu T, Zhang J, Gray NS, Smithgall TE, Engen JR. Conformational disturbance in Abl kinase upon mutation and deregulation. Proceedings of the National Academy of Sciences of the United States of America. 106: 1386-91. PMID 19164531 DOI: 10.1073/pnas.0811912106  1
2009 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. The Journal of Biological Chemistry. 284: 8023-32. PMID 19150980 DOI: 10.1074/jbc.M900301200  1
2009 Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nature Reviews. Cancer. 9: 28-39. PMID 19104514 DOI: 10.1038/nrc2559  1
2009 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. 127: 103-15. PMID 18793216 DOI: 10.1111/j.1365-2567.2008.02928.x  0.56
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, et al. Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature. 455: 975-8. PMID 18923525 DOI: 10.1038/nature07397  1
2008 Azam M, Seeliger MA, Gray NS, Kuriyan J, Daley GQ. Activation of tyrosine kinases by mutation of the gatekeeper threonine Nature Structural and Molecular Biology. 15: 1109-1118. PMID 18794843 DOI: 10.1038/nsmb.1486  1
2008 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, et al. Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. Bioorganic & Medicinal Chemistry Letters. 18: 5618-21. PMID 18793846 DOI: 10.1016/j.bmcl.2008.08.104  1
2008 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, ... ... Gray NS, et al. Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorganic & Medicinal Chemistry Letters. 18: 5916-9. PMID 18667312 DOI: 10.1016/j.bmcl.2008.07.062  1
2008 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, ... ... Gray NS, et al. EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 14: 4275-83. PMID 18594010 DOI: 10.1158/1078-0432.CCR-08-0168  1
2008 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, et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proceedings of the National Academy of Sciences of the United States of America. 105: 9059-64. PMID 18579783 DOI: 10.1073/pnas.0802982105  1
2008 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, ... ... Gray N, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nature Chemical Biology. 4: 347-56. PMID 18454143 DOI: 10.1038/nchembio.87  1
2008 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, et al. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Research. 68: 3389-95. PMID 18451166 DOI: 10.1158/0008-5472.CAN-07-6186  0.88
2008 Goldstein DM, Gray NS, Zarrinkar PP. High-throughput kinase profiling as a platform for drug discovery. Nature Reviews. Drug Discovery. 7: 391-7. PMID 18404149 DOI: 10.1038/nrd2541  1
2008 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 Chemical Biology. 3: 180-92. PMID 18307303 DOI: 10.1021/cb700200w  1
2008 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. The Journal of Biological Chemistry. 283: 29-36. PMID 17951261 DOI: 10.1074/jbc.M703988200  1
2007 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, ... ... Gray NS, et al. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proceedings of the National Academy of Sciences of the United States of America. 104: 19936-41. PMID 18077425 DOI: 10.1073/pnas.0707498104  1
2007 Peters EC, Gray NS. Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. Acs Chemical Biology. 2: 661-4. PMID 18041816 DOI: 10.1021/cb700203j  0.8
2007 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 Journal of Medicinal Chemistry. 50: 5875-5877. PMID 17975906 DOI: 10.1021/jm700983a  1
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 Chemical Biology. 2: 171-5. PMID 17348628 DOI: 10.1021/cb600435t  1
2007 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, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proceedings of the National Academy of Sciences of the United States of America. 104: 270-5. PMID 17185414 DOI: 10.1073/pnas.0609412103  1
2006 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, ... ... Gray N, et al. A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chemistry & Biology. 13: 1227-34. PMID 17114004 DOI: 10.1016/j.chembiol.2006.09.017  1
2006 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. Chemistry & Biology. 13: 779-86. PMID 16873026 DOI: 10.1016/j.chembiol.2006.05.015  1
2006 Liu Y, Gray NS. Rational design of inhibitors that bind to inactive kinase conformations. Nature Chemical Biology. 2: 358-64. PMID 16783341 DOI: 10.1038/nchembio799  1
2006 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, ... ... Gray N, et al. Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorganic & Medicinal Chemistry Letters. 16: 2689-92. PMID 16524731 DOI: 10.1016/j.bmcl.2006.02.032  1
2006 Nagle A, Hur W, Gray NS. Antimitotic agents of natural origin. Current Drug Targets. 7: 305-26. PMID 16515529  0.96
2006 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, ... ... Gray NS, et al. An efficient rapid system for profiling the cellular activities of molecular libraries. Proceedings of the National Academy of Sciences of the United States of America. 103: 3153-8. PMID 16492761 DOI: 10.1073/pnas.0511292103  1
2006 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. Journal of the American Chemical Society. 128: 2182-3. PMID 16478150 DOI: 10.1021/ja0567485  1
2006 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. Bioorganic & Medicinal Chemistry Letters. 16: 2173-6. PMID 16458503 DOI: 10.1016/j.bmcl.2006.01.053  1
2006 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 Nature Chemical Biology. 2: 95-102. PMID 16415863 DOI: 10.1038/nchembio760  1
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. Bioorganic & Medicinal Chemistry Letters. 15: 5467-73. PMID 16199156 DOI: 10.1016/j.bmcl.2005.08.097  1
2005 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. The Journal of Biological Chemistry. 280: 31220-9. PMID 15985434 DOI: 10.1074/jbc.M500805200  1
2005 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, ... ... Gray N, et al. Roscovitine targets, protein kinases and pyridoxal kinase. The Journal of Biological Chemistry. 280: 31208-19. PMID 15975926 DOI: 10.1074/jbc.M500806200  1
2005 Luesch H, Wu TY, Ren P, Gray NS, Schultz PG, Supek F. A genome-wide overexpression screen in yeast for small-molecule target identification. Chemistry & Biology. 12: 55-63. PMID 15664515 DOI: 10.1016/j.chembiol.2004.10.015  1
2004 Li B, Liu Y, Uno T, Gray N. Creating chemical diversity to target protein kinases. Combinatorial Chemistry & High Throughput Screening. 7: 453-72. PMID 15320712  1
2004 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. Chemistry & Biology. 11: 247-59. PMID 15123286 DOI: 10.1016/j.chembiol.2004.01.015  1
2004 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. Chemistry & Biology. 11: 135-46. PMID 15113003 DOI: 10.1016/S1074-5521(03)00298-9  1
2004 Wu X, Ding S, Ding Q, Gray NS, Schultz PG. Small molecules that induce cardiomyogenesis in embryonic stem cells. Journal of the American Chemical Society. 126: 1590-1. PMID 14871063 DOI: 10.1021/ja038950i  1
2004 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. The Journal of Biological Chemistry. 279: 13839-48. PMID 14732717 DOI: 10.1074/jbc.M311743200  1
2003 Gray NS. Optimization of experimental antimitotic agents: classical and combinatorial methods. Progress in Cell Cycle Research. 5: 135-43. PMID 14593707  1
2003 Warmuth M, Damoiseaux R, Liu Y, Fabbro D, Gray N. SRC family kinases: potential targets for the treatment of human cancer and leukemia. Current Pharmaceutical Design. 9: 2043-59. PMID 14529415  1
2003 Ding S, Wu TY, Brinker A, Peters EC, Hur W, Gray NS, Schultz PG. Synthetic small molecules that control stem cell fate. Proceedings of the National Academy of Sciences of the United States of America. 100: 7632-7. PMID 12794184 DOI: 10.1073/pnas.0732087100  1
2003 Ruetz S, Fabbro D, Zimmermann J, Meyer T, Gray N. Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. Current Medicinal Chemistry. Anti-Cancer Agents. 3: 1-14. PMID 12678910  0.36
2003 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. Molecular and Cellular Biology. 23: 831-41. PMID 12529389 DOI: 10.1128/MCB.23.3.831-841.2003  1
2002 Wu X, Ding S, Ding Q, Gray NS, Schultz PG. A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. Journal of the American Chemical Society. 124: 14520-1. PMID 12465946  1
2002 Knockaert M, Lenormand P, Gray N, Schultz P, Pouysségur J, Meijer L. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 21: 6413-24. PMID 12226745 DOI: 10.1038/sj.onc.1205908  0.44
2002 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 : a European Journal of Chemical Biology. 3: 897-901. PMID 12210991 DOI: 10.1002/1439-7633(20020902)3:9<897::AID-CBIC897>3.0.CO;2-B  1
2002 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. Journal of Virology. 76: 7874-82. PMID 12097601 DOI: 10.1128/JVI.76.15.7874-7882.2002  1
2002 Ding S, Gray NS, Ding Q, Wu X, Schultz PG. Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. Journal of Combinatorial Chemistry. 4: 183-6. PMID 11886295  1
2002 Ding S, Gray NS, Wu X, Ding Q, Schultz PG. A combinatorial scaffold approach toward kinase-directed heterocycle libraries. Journal of the American Chemical Society. 124: 1594-6. PMID 11853431  1
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. Journal of Medicinal Chemistry. 44: 4497-500. PMID 11741468 DOI: 10.1021/jm010451+  1
2001 Ding S, Gray NS, Ding Q, Schultz PG. A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines. The Journal of Organic Chemistry. 66: 8273-6. PMID 11722241  1
2001 Wu TY, Ding S, Gray NS, Schultz PG. Solid-phase synthesis of 2,3,5-trisubstituted indoles. Organic Letters. 3: 3827-30. PMID 11720546  1
2001 Lin Q, Jiang F, Schultz PG, Gray NS. Design of allele-specific protein methyltransferase inhibitors Journal of the American Chemical Society. 123: 11608-11613. PMID 11716715 DOI: 10.1021/ja011423j  1
2001 Gray NS. Combinatorial libraries and biological discovery Current Opinion in Neurobiology. 11: 608-614. PMID 11595496 DOI: 10.1016/S0959-4388(00)00257-9  1
2001 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. Journal of Medicinal Chemistry. 44: 2683-6. PMID 11495578 DOI: 10.1021/jm010171u  1
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. 407: 395-401. PMID 11014197 DOI: 10.1038/35030148  1
2000 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 We thank Sharon Long and Dave Keating for providing both the NodH sulfotransferase and APS Kinase during our preliminary experiments and Jack Kirsch for numerous helpful conversations. J.I.A. and K.G.B were supported by NIH Molecular Biophysics Training Grant (No. T32GM0895). This research was funded by grants to C.R.B. from the Pew Scholars Program, the W. M. Keck Foundation and the American Cancer Society (Grant No. RPG9700501BE). Angewandte Chemie (International Ed. in English). 39: 1303-1306. PMID 10767039 DOI: 10.1002/(SICI)1521-3773(20000403)39:7<1303::AID-ANIE1303>3.0.CO;2-0  1
1999 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. Chemistry & Biology. 6: 361-75. PMID 10375538 DOI: 10.1016/S1074-5521(99)80048-9  1
1999 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. Proceedings of the National Academy of Sciences of the United States of America. 96: 4797-802. PMID 10220373 DOI: 10.1073/pnas.96.9.4797  1
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 (New York, N.Y.). 281: 533-8. PMID 9677190 DOI: 10.1126/science.281.5376.533  1
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. The Journal of Biological Chemistry. 272: 29207-11. PMID 9360999  1
1996 Patten PA, Gray NS, Yang PL, Marks CB, Wedemayer GJ, Boniface JJ, Stevens RC, Schultz PG. The immunological evolution of catalysis. Science (New York, N.Y.). 271: 1086-91. PMID 8599084  1
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