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Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y, Choi HG, Xie T, Deng X, Buhrlage SJ, Sim T, Cohen P, Sapkota G, Westover KD, Gray NS. Tan L, et al. Among authors: sim t. J Med Chem. 2015 Jan 8;58(1):183-96. doi: 10.1021/jm500480k. Epub 2014 Jul 30. J Med Chem. 2015. PMID: 25075558 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
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
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
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. Zhang G, et al. Among authors: sim t. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5618-21. doi: 10.1016/j.bmcl.2008.08.104. Epub 2008 Aug 31. Bioorg Med Chem Lett. 2008. PMID: 18793846
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
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. Zhang G, et al. Among authors: sim t. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6691-5. doi: 10.1016/j.bmcl.2009.09.123. Epub 2009 Oct 12. Bioorg Med Chem Lett. 2009. PMID: 19854052
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.
384 results