Publications

2010

Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray NS, Wilner K, Christensen JG, Demetri G, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA. The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.  Cancer Res. 2010;70(24):10038-43.

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Chen Z, Sasaki T, Tan X, Carretero J, Shimamura T, Li D, Xu C, Wang Y, Adelmant GO, Capelletti M, Lee HJ, Rodig SJ, Borgman C, Park SI, Kim HR, Padera R, Marto JA, Gray NS, Kung AL, Shapiro GI, Jänne PA, Wong KK.  Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene.  Cancer Res. 2010;70(23):9827-36.

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Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS.  Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.  J Med Chem. 2010;53(19):7146-55.

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Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR 3rd, Gray NS, Lee JD  Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010;18(3):258-67. Erratum in: Cancer Cell. 2010;18(4):396. 

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Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS.  Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem. 2010;53(19):6934-46.

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Weisberg E, Choi HG, Barrett R, Zhou W, Zhang J, Ray A, Nelson EA, Jiang J, Moreno D, Stone R, Galinsky I, Fox E, Adamia S, Kung AL, Gray NS, Griffin JD.  Discovery and characterization of novel mutant FLT3 kinase inhibitors.  Mol Cancer Ther. 2010;9(9):2468-77.

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Deng X, Nagle A, Wu T, Sakata T, Henson K, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Tully DC, Chatterjee AK, Gray NS.  Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.  Bioorg Med Chem Lett. 2010;20(14):4027-31.

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Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T.  A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.  J Med Chem. 2010;53(15):5439-48.

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Deng X, Lim SM, Zhang J, Gray NS.  Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.  Bioorg Med Chem Lett. 2010;20(14):4196-200.

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Hur W, Sun Z, Jiang T, Mason DE, Peters EC, Zhang DD, Luesch H, Schultz PG, Gray NS. A small-molecule inducer of the antioxidant response element.  Chem Biol. 2010;17(5):537-47.

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Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010; 6(5):359-68.

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Zhou W, Hur W, Mc Dermott 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;17(3):285-95.

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Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, 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. Disvoery pf small molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR Kit,a nd Srckinase. Blood. 2010;115(21):4206-16.

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Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fenrich 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;1804(3):454-62.

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McDermott U, Pusapati RV, Christensen JG, Gray NS, Settleman J. Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res. 2010;70(4):1625-34.

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Zhang J., Adrián, FJ, Jahnke W, Cowan-Jacob SW, Allen G. Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun G, 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 wild-type and T315I Bcr-Abl by combining allosteric with ATP-site inhibitors. Nature. 2010;463(7280):501-6.

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