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The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance.
Yang G, Wang J, Tan L, Munshi M, Liu X, Kofides A, Chen JG, Tsakmaklis N, Demos MG, Guerrera ML, Xu L, Hunter ZR, Che J, Patterson CJ, Meid K, Castillo JJ, Munshi NC, Anderson KC, Cameron M, Buhrlage SJ, Gray NS, Treon SP. Yang G, et al. Among authors: gray ns. Blood. 2021 Nov 18;138(20):1966-1979. doi: 10.1182/blood.2021011405. Blood. 2021. PMID: 34132782 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.
mTOR Mediated Anti-Cancer Drug Discovery.
Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. Liu Q, et al. Among authors: gray ns. 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.
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: gray ns. J Med Chem. 2011 Mar 10;54(5):1473-80. doi: 10.1021/jm101520v. Epub 2011 Feb 15. J Med Chem. 2011. PMID: 21322566 Free PMC article.
A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors.
Sasaki T, Koivunen J, Ogino A, Yanagita M, Nikiforow S, Zheng W, Lathan C, Marcoux JP, Du J, Okuda K, Capelletti M, Shimamura T, Ercan D, Stumpfova M, Xiao Y, Weremowicz S, Butaney M, Heon S, Wilner K, Christensen JG, Eck MJ, Wong KK, Lindeman N, Gray NS, Rodig SJ, Jänne PA. Sasaki T, et al. Among authors: gray ns. Cancer Res. 2011 Sep 15;71(18):6051-60. doi: 10.1158/0008-5472.CAN-11-1340. Epub 2011 Jul 26. Cancer Res. 2011. PMID: 21791641 Free PMC article.
560 results