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Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Khanna A, Côté A, Arora S, Moine L, Gehling VS, Brenneman J, Cantone N, Stuckey JI, Apte S, Ramakrishnan A, Bruderek K, Bradley WD, Audia JE, Cummings RT, Sims RJ 3rd, Trojer P, Levell JR. Khanna A, et al. Among authors: bradley wd. ACS Med Chem Lett. 2020 Mar 26;11(6):1205-1212. doi: 10.1021/acsmedchemlett.0c00045. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551002 Free PMC article.
Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation.
Su F, Bradley WD, Wang Q, Yang H, Xu L, Higgins B, Kolinsky K, Packman K, Kim MJ, Trunzer K, Lee RJ, Schostack K, Carter J, Albert T, Germer S, Rosinski J, Martin M, Simcox ME, Lestini B, Heimbrook D, Bollag G. Su F, et al. Among authors: bradley wd. Cancer Res. 2012 Feb 15;72(4):969-78. doi: 10.1158/0008-5472.CAN-11-1875. Epub 2011 Dec 28. Cancer Res. 2012. PMID: 22205714
EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.
Bradley WD, Arora S, Busby J, Balasubramanian S, Gehling VS, Nasveschuk CG, Vaswani RG, Yuan CC, Hatton C, Zhao F, Williamson KE, Iyer P, Méndez J, Campbell R, Cantone N, Garapaty-Rao S, Audia JE, Cook AS, Dakin LA, Albrecht BK, Harmange JC, Daniels DL, Cummings RT, Bryant BM, Normant E, Trojer P. Bradley WD, et al. Chem Biol. 2014 Nov 20;21(11):1463-75. doi: 10.1016/j.chembiol.2014.09.017. Chem Biol. 2014. PMID: 25457180
21 results