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Targeting transcription regulation in cancer with a covalent CDK7 inhibitor.
Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS. Kwiatkowski N, et al. Among authors: sim t. Nature. 2014 Jul 31;511(7511):616-20. doi: 10.1038/nature13393. Epub 2014 Jun 22. Nature. 2014. PMID: 25043025 Free PMC article.
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
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. Adrián FJ, et al. Among authors: sim t. Nat Chem Biol. 2006 Feb;2(2):95-102. doi: 10.1038/nchembio760. Epub 2006 Jan 15. Nat Chem Biol. 2006. PMID: 16415863
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
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. Zhang J, et al. Among authors: sim t. Nature. 2010 Jan 28;463(7280):501-6. doi: 10.1038/nature08675. Epub 2010 Jan 13. Nature. 2010. PMID: 20072125 Free PMC article.
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
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. Kwiatkowski N, et al. Among authors: sim t. Nat Chem Biol. 2010 May;6(5):359-68. doi: 10.1038/nchembio.345. Epub 2010 Apr 11. Nat Chem Biol. 2010. PMID: 20383151 Free PMC article.
Expanding the diversity of allosteric bcr-abl inhibitors.
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. Deng X, et al. Among authors: sim t. J Med Chem. 2010 Oct 14;53(19):6934-46. doi: 10.1021/jm100555f. J Med Chem. 2010. PMID: 20828158 Free PMC article.
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.
Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: sim t. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f. J Med Chem. 2010. PMID: 20860370 Free PMC article.
384 results