Article
EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL.
Molecular cancer therapeutics - 1 Nov 2017
Brach Dorothy, Johnston-Blackwell Danielle, Drew Allison, Lingaraj Trupti, Motwani Vinny, Warholic Natalie M, Feldman Igor, Plescia Christopher, Smith Jesse J, Copeland Robert A, Keilhack Heike, Chan-Penebre Elayne, Knutson Sarah K, Ribich Scott A, Raimondi Alejandra, Thomenius Michael J
Abstract excerpt
The EZH2 small-molecule inhibitor tazemetostat (EPZ-6438) is currently being evaluated in phase II clinical trials for the treatment of non-Hodgkin lymphoma (NHL). We have previously shown that EZH2 inhibitors display an antiproliferative effect in multiple preclinical models of NHL, and that models bearing gain-of-function mutations in EZH2 were consistently more sensitive to EZH2 inhibition than lymphomas with...
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