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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
A general strategy for creating "inactive-conformation" abl inhibitors.
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. Okram B, et al. Among authors: sim t. Chem Biol. 2006 Jul;13(7):779-86. doi: 10.1016/j.chembiol.2006.05.015. Chem Biol. 2006. PMID: 16873026
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.
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.
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 PW, Adamia S, Wu C, Gray N, Griffin JD. Weisberg E, et al. Among authors: sim t. Blood. 2010 May 27;115(21):4206-16. doi: 10.1182/blood-2009-11-251751. Epub 2010 Mar 18. Blood. 2010. PMID: 20299508 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.
383 results