• Home
  • News
  • Calendar
  • About DF/HCC
  • Membership
  • Visitor Center

Nathanael Gray, PhD

Publications

  • Vetter ML, Zhang Z, Liu S, Wang J, Cho H, Zhang J, Zhang W, Gray NS, Yang PL.Fluorescent Visualization of Src by Using Dasatinib-BODIPY.Chembiochem. 2014 Jun 16;15(9):1317-24.
    24828915
  • Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, Xie T, Marto JA, Chen Z, Gray NS, Westover KD.In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C.Proc Natl Acad Sci U S A. 2014 Jun 2.
    24889603
  • Wang Y, Lee YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ.MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.Elife. 2014 May 20:e01763.
    24844244
  • Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS.Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?.ACS Chem Biol. 2014 Apr 29.
    24730530
  • Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN.Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors.J Mol Biol. 2014 Apr 22.
    24768818
  • Decker S, Finter J, Forde AJ, Kissel S, Schwaller J, Mack TS, Kuhn A, Gray N, Follo M, Jumaa H, Burger M, Zirlik K, Pfeifer D, Miduturu CV, Eibel H, Veelken H, Dierks C.PIM Kinases Are Essential for Chronic Lymphocytic Leukemia Cell Survival (PIM2/3) and CXCR4-Mediated Microenvironmental Interactions (PIM1).Mol Cancer Ther. 2014 Apr 22.
    24659821
  • Amato KR, Wang S, Hastings AK, Youngblood VM, Santapuram PR, Chen H, Cates JM, Colvin DC, Ye F, Brantley-Sieders DM, Cook RS, Tan L, Gray NS, Chen J.Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC.J Clin Invest. 2014 Apr 8.
    24713656
  • Wu H, Wang W, Liu F, Weisberg EL, Tian B, Chen Y, Li B, Wang A, Wang B, Zhao Z, McMillin DW, Hu C, Li H, Wang J, Liang Y, Buhrlage SJ, Liang J, Liu J, Yang G, Brown JR, Treon SP, Mitsiades CS, Griffin JD, Liu Q, Gray NS.Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma.ACS Chem Biol. 2014 Mar 17.
    24556163
  • Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY.Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.J Med Chem. 2013 Jul 25;56(14):5675-90.
    23742252
  • Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS.Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.Biochem J. 2014 Jan 1;457(1):215-25.
    24171924
  • Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS.Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.Eur J Med Chem. 2013 Dec;70:758-67.
    24239623
  • 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.Mol Cancer Ther. 2013 Dec;12(12):2651-62.
    24130053
  • 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.Mol Cancer Ther. 2013 Dec 2.
    24296828
  • Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, Carrasco M, Hunter J, Kim ND, Xie T, Sim T, Jänne PA, Meyerson M, Marto JA, Engen JR, Gray NS.Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor.Angew Chem Int Ed Engl. 2013 Nov 20.
    24259466
  • Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell SA, Wu H, Zhao Z, Wang J, Mandinova A, Griffin JD, Bullock AN, Liu Q, Lee SW, Gray NS.Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
    23899692
  • Tannous BA, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, Geerts D, De Witt Hamer PC, Hagemann C, Vandertop WP, Van Tellingen O, Noske DP, Gray NS, Würdinger T.Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs.Journal of the National Cancer Institute. 2013 Sep 4;105(17):1322-31.
    23940287
  • Yang G, Zhou Y, Liu X, Xu L, Cao Y, Manning RJ, Patterson CJ, Buhrlage SJ, Gray N, Tai YT, Anderson KC, Hunter ZR, Treon SP.A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia.Blood. 2013 Aug 15;122(7):1222-32.
    23836557
  • Liao RG, Jung J, Tchaicha J, Wilkerson MD, Sivachenko A, Beauchamp EM, Liu Q, Pugh TJ, Pedamallu CS, Hayes DN, Gray NS, Getz G, Wong KK, Haddad RI, Meyerson M, Hammerman PS.Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma.Cancer Res. 2013 Aug 15;73(16):5195-205.
    23786770
  • Liu Y, Marks K, Cowley GS, Carretero J, Liu Q, Nieland TJ, Xu C, Cohoon TJ, Gao P, Zhang Y, Chen Z, Altabef AB, Tchaicha JH, Wang X, Choe S, Driggers EM, Zhang J, Bailey ST, Sharpless NE, Hayes DN, Patel NM, Janne PA, Bardeesy N, Engelman JA, Manning BD, Shaw RJ, Asara JM, Scully R, Kimmelman A, Byers LA, Gibbons DL, Wistuba II, Heymach JV, Kwiatkowski DJ, Kim WY, Kung AL, Gray NS, Root DE, Cantley LC, Wong KK.Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer.Cancer Discovery. 2013 Aug;3(8):870-9.
    23715154
  • Kang SA, Pacold ME, Cervantes CL, Lim D, Lou HJ, Ottina K, Gray NS, Turk BE, Yaffe MB, Sabatini DM.mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin.Science. 2013 Jul 26;341(6144):1236566.
    23888043
  • Taipale M, Krykbaeva I, Whitesell L, Santagata S, Zhang J, Liu Q, Gray NS, Lindquist S.Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells.Nat Biotechnol. 2013 Jul;31(7):630-7.
    23811600
  • Elkins JM, Wang J, Deng X, Pattison MJ, Arthur S, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S.X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor.J Med Chem. 2013 May 8.
    23656407
  • Sanda T, Tyner JW, Gutierrez A, Ngo VN, Glover J, Chang BH, Yost A, Ma W, Fleischman AG, Zhou W, Yang Y, Kleppe M, Ahn Y, Tatarek J, Kelliher MA, Neuberg DS, Levine RL, Moriggl R, Müller M, Gray NS, Jamieson CH, Weng AP, Staudt LM, Druker BJ, Look AT.TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia.Cancer Discovery. 2013 May;3(5):564-77.
    23471820
  • Liu F, Zhang X, Weisberg E, Chen S, Hur W, Wu H, Zhao Z, Wang W, Mao M, Cai C, Simon NI, Sanda T, Wang J, Look AT, Griffin JD, Balk SP, Liu Q, Gray NS.Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer.ACS Chem Biol. 2013 Apr 17.
    23594111
  • Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS.Characterization of Torin2, an ATP-Competitive Inhibitor of mTOR, ATM, and ATR.Cancer Res. 2013 Apr 15;73(8):2574-2586.
    23436801
  • Guo Y, Chekaluk Y, Zhang J, Du J, Gray NS, Wu CL, Kwiatkowski DJ.TSC1 involvement in bladder cancer: diverse effects and therapeutic implications.J Pathol. 2013 May;230(1):17-27.
    23401075
  • Weisberg E, Liu Q, Zhang X, Nelson E, Sattler M, Liu F, Nicolais M, Zhang J, Mitsiades C, Smith RW, Stone R, Galinsky I, Nonami A, Griffin JD, Gray N.Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells.PLoS ONE. 2013;8(2):e56473.
    23437141
  • Cortot AB, Repellin CE, Shimamura T, Capelletti M, Zejnullahu K, Ercan D, Christensen JG, Wong KK, Gray NS, Jänne PA.Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway.Cancer Res. 2013 Jan 15;73(2):834-43.
    23172312
  • Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ.A public-private partnership to unlock the untargeted kinome.Nat Chem Biol. 2013 Jan;9(1):3-6.
    23238671
  • Clark K, Mackenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E, Gray NS, Arthur JS, Cohen P.Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.
    23033494
  • Ercan D, Xu C, Yanagita M, Monast CS, Pratilas CA, Montero J, Butaney M, Shimamura T, Sholl L, Ivanova EV, Tadi M, Rogers A, Repellin C, Capelletti M, Maertens O, Goetz EM, Letai A, Garraway LA, Lazzara MJ, Rosen N, Gray NS, Wong KK, Jänne PA.Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.Cancer Discovery. 2012 Oct;2(10):934-47.
    22961667
  • Duan Z, Zhang J, Choy E, Harmon D, Liu X, Nielsen P, Mankin H, Gray NS, Hornicek FJ.Systematic Kinome shRNA Screening Identifies CDK11 (PITSLRE) Kinase Expression Is Critical for Osteosarcoma Cell Growth and Proliferation.Clin Cancer Res. 2012 Sep 1;18(17):4580-8.
    22791884
  • Zhang Z, Kwiatkowski N, Zeng H, Lim SM, Gray NS, Zhang W, Yang PL.Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy.Mol Biosyst. 2012 Oct;8(10):2523-6.
    22673640
  • Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS.GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.
    22863203
  • Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW.Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma.Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12722-7.
    22802621
  • Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS.Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.Bioorg Med Chem Lett. 2012 Aug 15;22(16):5297-302.
    22819762
  • Lau KS, Zhang T, Kendall KR, Lauffenburger D, Gray NS, Haigis KM.BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner.PLoS ONE. 2012;7(7):e41343.
    22815993
  • Berry T, Luther W, Bhatnagar N, Jamin Y, Poon E, Sanda T, Pei D, Sharma B, Vetharoy WR, Hallsworth A, Ahmad Z, Barker K, Moreau L, Webber H, Wang W, Liu Q, Perez-Atayde A, Rodig S, Cheung NK, Raynaud F, Hallberg B, Robinson SP, Gray NS, Pearson AD, Eccles SA, Chesler L, George RE.The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.Cancer Cell. 2012 Jul 10;22(1):117-30.
    22789543
  • 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.Bioorg Med Chem Lett. 2012 Jul 15;22(14):4579-84.
    22727638
  • Liu Q, Ren T, Fresques T, Oppliger W, Niles BJ, Hur W, Sabatini DM, Hall MN, Powers T, Gray NS.Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae.ACS Chem Biol. 2012 Jun 15;7(6):982-7.
    22496512
  • Haber DA, Gray NS, Baselga J.The evolving war on cancer.Cell. 2011 Apr 1;145(1):19-24.
    21458664
  • 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. 2011 Mar 10;2(3):195-200.
    21412406
  • Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS.Discovery of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a Potent, Selective, and Orally Available Mammalian Target of Rapamycin (mTOR) Inhibitor for Treatment of Cancer.J Med Chem. 2011 Mar 10;54(5):1473-80.
    21322566
  • Hur W, Gray NS.Small molecule modulators of antioxidant response pathway.Curr Opin Chem Biol. 2011 Feb;15(1):162-73.
    21195017
  • Iacob RE, Zhang J, Gray NS, Engen JR.Allosteric interactions between the myristate- and ATP-site of the Abl kinase.PLoS ONE. 2011;6(1):e15929.
    21264348
  • Zhou W, Ercan D, Jänne PA, Gray NS.Discovery of selective irreversible inhibitors for EGFR-T790M.Bioorg Med Chem Lett. 2011 Jan 15;21(2):638-43.
    21208802
  • Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray NS, Wilner K, Christensen JG, Demetri G, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA.The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.Cancer Res. 2010 Dec 15;70(24):10038-43.
    21030459
  • Chen Z, Sasaki T, Tan X, Carretero J, Shimamura T, Li D, Xu C, Wang Y, Aldelmant GO, Capelletti M, Lee HJ, Rodig SJ, Borgman CL, Park SI, Kim HR, Padera RF, Marto J, Gray N, Kung AL, Shapiro GI, Janne PA, Wong KK.Inhibition of ALK, PI3K/MEK and HSP90 in Murine Lung Adenocarcinoma Induced by EML4-ALK Fusion Oncogene.Cancer Res. 2010 Dec 1;70(23):9827-36.
    20952506
  • Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS.Expanding the diversity of allosteric bcr-abl inhibitors.J Med Chem. 2010 Oct 14;53(19):6934-46.
    20828158
  • Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS.Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly potent, selective mammalian target of Rapamycin (mTOR) inhibitor for the treatment of cancer.J Med Chem. 2010 Oct 14;53(19):7146-55.
    20860370
  • Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR, Gray NS, Lee JD.Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.Cancer Cell. 2010 Sep 14;18(3):258-67.
    20832753
  • Weisberg E, Choi HG, Barrett R, Zhou W, Zhang J, Ray A, Nelson EA, Jiang J, Moreno D, Stone R, Galinsky I, Fox E, Adamia S, Kung AL, Gray NS, Griffin JD.Discovery and characterization of novel mutant FLT3 kinase inhibitors.Mol Cancer Ther. 2010 Sep;9(9):2468-77.
    20807780
  • Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T.A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.J Med Chem. 2010 Aug 12;53(15):5439-48.
    20604564
  • Deng X, Lim SM, Zhang J, Gray NS.Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.Bioorg Med Chem Lett. 2010 Jul 15;20(14):4196-200.
    20541934
  • Hur W, Sun Z, Jiang T, Mason DE, Peters EC, Zhang DD, Luesch H, Schultz PG, Gray NS.A small-molecule inducer of the antioxidant response element.Chem Biol. 2010 May 28;17(5):537-47.
    20534351
  • Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, Sim T, Zhou W, Seeliger M, Cameron M, Azam M, Fletcher JA, Debiec-Rychter M, Mayeda M, Moreno D, Kung AL, Janne PA, Khosravi-Far R, Melo JV, Manley P, Adamia S, Wu C, Gray N, Griffin JD.Discovery of a small molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR{alpha}, Kit, and Src kinases.Blood. 2010 May 27;115(21):4206-16.
    20299508
  • Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS.Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.Nat Chem Biol. 2010 May;6(5):359-68.
    20383151
  • Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS.A structure-guided approach to creating covalent FGFR inhibitors.Chem Biol. 2010 Mar 26;17(3):285-95.
    20338520
  • McDermott U, Pusapati RV, Christensen JG, Gray NS, Settleman J.Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency.Cancer Res. 2010 Feb 15;70(4):1625-34.
    20124471
  • Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J.Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.Biochim Biophys Acta. 2010 Mar;1804(3):454-62.
    20152788
  • Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS.Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.Nature. 2010 Jan 28;463(7280):501-6.
    20072125
  • Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA.Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4.
    20033049
  • Emery CM, Vijayendran KG, Zipser MC, Sawyer AM, Niu L, Kim JJ, Hatton C, Chopra R, Oberholzer PA, Karpova MB, MacConaill LE, Zhang J, Gray NS, Sellers WR, Dummer R, Garraway LA.MEK1 mutations confer resistance to MEK and B-RAF inhibition.Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20411-6.
    19915144
  • Zhang G, Ren P, Gray NS, Sim T, Wang X, Liu Y, Che J, Dong W, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Wang Z, Seidel HM, Karanewsky DS, He Y.Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.Bioorg Med Chem Lett. 2009 Dec 1;19(23):6691-5.
    19854052
  • Choi Y, Seeliger MA, Panjarian SB, Kim H, Deng X, Sim T, Couch B, Koleske AJ, Smithgall TE, Gray NS.N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor.J Biol Chem. 2009 Oct 16;284(42):29005-14.
    19679652
  • Jänne PA, Gray N, Settleman J.Factors underlying sensitivity of cancers to small-molecule kinase inhibitors.Nat Rev Drug Discov. 2009 Sep;8(9):709-23. Review.
    19629074
  • Choi Y, Syeda F, Walker JR, Finerty PJ, Cuerrier D, Wojciechowski A, Liu Q, Dhe-Paganon S, Gray NS.Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors.Bioorg Med Chem Lett. 2009 Aug 1;19(15):4467-70.
    19553108
  • Weisberg E,Barrett R,Liu Q,Stone R,Gray N,Griffin JD.FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML.Drug Resist Updat. 2009 Jun;12(3):81-9. Review.
    19467916
  • Peterson TR,Laplante M,Thoreen CC,Sancak Y,Kang SA,Kuehl WM,Gray NS,Sabatini DM.DEPTOR Is an mTOR Inhibitor Frequently Overexpressed in Multiple Myeloma Cells and Required for Their Survival.Cell. 2009 May 29;137(5):873-86.
    19446321
  • Xian W,Pappas L,Pandya D,Selfors LM,Derksen PW,de Bruin M,Gray NS,Jonkers J,Rosen JM,Brugge JS.Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival.Cancer Res. 2009 Mar 15;69(6):2244-51.
    19258500
  • Avni D,Goldsmith M,Ernst O,Mashiach R,Tuntland T,Meijler MM,Gray NS,Rosen H,Zor T.Modulation of TNFalpha, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages.Immunol Lett. 2009 Mar 24;123(1):1-8.
    19185589
  • Saenz JB,Sun WJ,Chang JW,Li J,Bursulaya B,Gray NS,Haslam DB.Golgicide A reveals essential roles for GBF1 in Golgi assembly and function.Nat Chem Biol. 2009 Mar;5(3):157-65.
    19182783
  • Iacob RE,Pene-Dumitrescu T,Zhang J,Gray NS,Smithgall TE,Engen JR.Conformational disturbance in Abl kinase upon mutation and deregulation.Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1386-91.
    19164531
  • Thoreen CC,Kang SA,Chang JW,Liu Q,Zhang J,Gao Y,Reichling LJ,Sim T,Sabatini DM,Gray NS.An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1.J Biol Chem. 2009 Mar 20;284(12):8023-32.
    19150980
  • Zhang J,Yang PL,Gray NS.Targeting cancer with small molecule kinase inhibitors.Nat Rev Cancer. 2009 Jan;9(1):28-39. Review.
    19104514
  • George RE,Sanda T,Hanna M,Frohling S,Luther W 2nd,Zhang J,Ahn Y,Zhou W,London WB,McGrady P,Xue L,Zozulya S,Gregor VE,Webb TR,Gray NS,Gilliland DG,Diller L,Greulich H,Morris SW,Meyerson M,Look AT.Activating mutations in ALK provide a therapeutic target in neuroblastoma.Nature. 2008 Oct 16;455(7215):975-8.
    18923525
  • Goldsmith M,Avni D,Levy-Rimler G,Mashiach R,Ernst O,Levi M,Webb B,Meijler MM,Gray NS,Rosen H,Zor T.A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages.Immunology. 2009 May;127(1):103-15.
    18793216
  • Zhang G,Ren P,Gray NS,Sim T,Liu Y,Wang X,Che J,Tian SS,Sandberg ML,Spalding TA,Romeo R,Iskandar M,Chow D,Martin Seidel H,Karanewsky DS,He Y.Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.Bioorg Med Chem Lett. 2008 Oct 15;18(20):5618-21.
    18793846
  • Azam M,Seeliger MA,Gray NS,Kuriyan J,Daley GQ.Activation of tyrosine kinases by mutation of the gatekeeper threonine.Nat Struct Mol Biol. 2008 Oct;15(10):1109-18.
    18794843
  • Hur W,Velentza A,Kim S,Flatauer L,Jiang X,Valente D,Mason DE,Suzuki M,Larson B,Zhang J,Zagorska A,Didonato M,Nagle A,Warmuth M,Balk SP,Peters EC,Gray NS.Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9.
    18667312
  • Koivunen JP,Mermel C,Zejnullahu K,Murphy C,Lifshits E,Holmes AJ,Choi HG,Kim J,Chiang D,Thomas R,Lee J,Richards WG,Sugarbaker DJ,Ducko C,Lindeman N,Marcoux JP,Engelman JA,Gray NS,Lee C,Meyerson M,Janne PA.EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer.Clin Cancer Res. 2008 Jul 1;14(13):4275-83.
    18594010
  • Kato N, Sakata T, Breton G, Le Roch KG, Nagle A, Andersen C, Bursulaya B, Henson K, Johnson J, Kumar KA, Marr F, Mason D, McNamara C, Plouffe D, Ramachandran V, Spooner M, Tuntland T, Zhou Y, Peters EC, Chatterjee A, Schultz PG, Ward GE, Gray N, Harper J, Winzeler EA.Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.Nat Chem Biol. 2008 Jun;4(6):347-56.
    18454143
  • McDermott U, Iafrate AJ, Gray NS, Shioda T, Classon M, Maheswaran S, Zhou W, Choi HG, Smith SL, Dowell L, Ulkus LE, Kuhlmann G, Greninger P, Christensen JG, Haber DA, Settleman J.Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors.Cancer Res. 2008 May 1;68(9):3389-95.
    18451166
  • Goldstein DM, Gray NS, Zarrinkar PP.High-throughput kinase profiling as a platform for drug discovery.Nat Rev Drug Discov. 2008 May;7(5):391-7. Review.
    18404149
  • Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS.Discovery of selective aminothiazole aurora kinase inhibitors.ACS Chem Biol. 2008 Mar 20;3(3):180-92.
    18307303
  • McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J.Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41.
    18077425
  • Peters EC, Gray NS.Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors.ACS Chem Biol. 2007 Oct 19;2(10):661-4.
    18041816
  • Jansma A, Zhang Q, Li B, Ding Q, Uno T, Bursulaya B, Liu Y, Furet P, Gray NS, Geierstanger BH.Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy.J Med Chem. 2007 Nov 29;50(24):5875-7.
    17975906
  • Supekova L, Supek F, Lee J, Chen S, Gray N, Pezacki JP, Schlapbach A, Schultz PG.Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening.J Biol Chem. 2008 Jan 4;283(1):29-36.
    17951261
  • Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, Gray NS, Warmuth M.Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5.
    17185414
  • Okram B, Nagle A, Adrin FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS.A general strategy for creating "inactive-conformation" abl inhibitors.Chem Biol. 2006 Jul;13(7):779-86.
    16873026
  • Liu Y, Gray NS.Rational design of inhibitors that bind to inactive kinase conformations.Nat Chem Biol. 2006 Jul;2(7):358-64.
    16783341
  • Melnick JS, Janes J, Kim S, Chang JY, Sipes DG, Gunderson D, Jarnes L, Matzen JT, Garcia ME, Hood TL, Beigi R, Xia G, Harig RA, Asatryan H, Yan SF, Zhou Y, Gu XJ, Saadat A, Zhou V, King FJ, Shaw CM, Su AI, Downs R, Gray NS, Schultz PG, Warmuth M, Caldwell JS.An efficient rapid system for profiling the cellular activities of molecular libraries.Proc Natl Acad Sci U S A. 2006 Feb 28;103(9):3153-8.
    16492761
  • Adrin FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P, Mestan J, Fabbro D, Gray NS.Allosteric inhibitors of Bcr-abl-dependent cell proliferation.Nat Chem Biol. 2006 Feb;2(2):95-102.
    16415863