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Page 1
mTOR Mediated Anti-Cancer Drug Discovery.
Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. Liu Q, et al. Drug Discov Today Ther Strateg. 2009 Summer;6(2):47-55. doi: 10.1016/j.ddstr.2009.12.001. Drug Discov Today Ther Strateg. 2009. PMID: 20622997 Free PMC article.
A structure-guided approach to creating covalent FGFR inhibitors.
Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS. Zhou W, et al. Chem Biol. 2010 Mar 26;17(3):285-95. doi: 10.1016/j.chembiol.2010.02.007. Chem Biol. 2010. PMID: 20338520 Free PMC article.
Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.
Deng X, Lim SM, Zhang J, Gray NS. Deng X, et al. 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.
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS. Hur W, et al. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9. doi: 10.1016/j.bmcl.2008.07.062. Epub 2008 Jul 18. Bioorg Med Chem Lett. 2008. PMID: 18667312 Free PMC article.
In situ kinase profiling reveals functionally relevant properties of native kinases.
Patricelli MP, Nomanbhoy TK, Wu J, Brown H, Zhou D, Zhang J, Jagannathan S, Aban A, Okerberg E, Herring C, Nordin B, Weissig H, Yang Q, Lee JD, Gray NS, Kozarich JW. Patricelli MP, et al. Chem Biol. 2011 Jun 24;18(6):699-710. doi: 10.1016/j.chembiol.2011.04.011. Chem Biol. 2011. PMID: 21700206 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. 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.