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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. Nature. 2010 Jan 28;463(7280):501-6. doi: 10.1038/nature08675. Epub 2010 Jan 13. Nature. 2010. PMID: 20072125 Free PMC article.
Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.
Deng X, Lim SM, Zhang J, Gray NS. Deng X, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4196-200. doi: 10.1016/j.bmcl.2010.05.043. Epub 2010 May 19. Bioorg Med Chem Lett. 2010. PMID: 20541934 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: zhang g, zhang j. J Med Chem. 2010 Oct 14;53(19):6934-46. doi: 10.1021/jm100555f. J Med Chem. 2010. PMID: 20828158 Free PMC article.
Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.
Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS. Choi HG, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5297-302. doi: 10.1016/j.bmcl.2012.06.036. Epub 2012 Jun 23. Bioorg Med Chem Lett. 2012. PMID: 22819762 Free PMC article.
Conformational disturbance in Abl kinase upon mutation and deregulation.
Iacob RE, Pene-Dumitrescu T, Zhang J, Gray NS, Smithgall TE, Engen JR. Iacob RE, et al. Among authors: zhang j. Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1386-91. doi: 10.1073/pnas.0811912106. Epub 2009 Jan 21. Proc Natl Acad Sci U S A. 2009. PMID: 19164531 Free PMC article.
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
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. Fabbro D, et al. Among authors: zhang j. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
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: zhang j. 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.
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