Nathanael Gray, PhD

Publications

• 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-
  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 Rapamy
  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-trans
  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 M
  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, selecti
  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):2
  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 C
  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
  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
  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-
  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
  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 Sc
  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
  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
  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):224
  19258500
• 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
• 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
• 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
  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 macropha
  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(2
  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
  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,
  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 an
  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, S
  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 Sc
  17185414
• Okram B, Nagle A, Adrián FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS.A general strategy for creating "inactive-conformation" abl inhibitors.Chem Biol. 2006 Jul;13(7):779-86.
  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
  16492761
• Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P, Mestan J, Fabbro D, Gray NS.Allosteric inhibitors of Bcr-abl-dependent cell proliferation.Nat Chem Biol. 2006 Feb;2(2):95-102.
  16415863