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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: gray ns. 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.
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: gray ns. Chem Biol. 2006 Jul;13(7):779-86. doi: 10.1016/j.chembiol.2006.05.015. Chem Biol. 2006. PMID: 16873026
EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer.
Koivunen JP, Mermel C, Zejnullahu K, Murphy C, Lifshits E, Holmes AJ, Choi HG, Kim J, Chiang D, Thomas R, Lee J, Richards WG, Sugarbaker DJ, Ducko C, Lindeman N, Marcoux JP, Engelman JA, Gray NS, Lee C, Meyerson M, Jänne PA. Koivunen JP, et al. Among authors: gray ns. Clin Cancer Res. 2008 Jul 1;14(13):4275-83. doi: 10.1158/1078-0432.CCR-08-0168. Clin Cancer Res. 2008. PMID: 18594010 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. Among authors: gray ns. 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.
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: gray ns. 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
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: gray ns. 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.
Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors.
Choi Y, Syeda F, Walker JR, Finerty PJ Jr, Cuerrier D, Wojciechowski A, Liu Q, Dhe-Paganon S, Gray NS. Choi Y, et al. Among authors: gray ns. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4467-70. doi: 10.1016/j.bmcl.2009.05.029. Epub 2009 May 13. Bioorg Med Chem Lett. 2009. PMID: 19553108 Free PMC article.
560 results