Article
Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors.
Oncotarget - 20 Oct 2015
Baker Theresa, Nerle Sujata, Pritchard Justin, Zhao Boyang, Rivera Victor M, Garner Andrew, Gonzalvez Francois
Abstract excerpt
Although targeted therapies have revolutionized cancer treatment, overcoming acquired resistance remains a major clinical challenge. EZH2 inhibitors (EZH2i), EPZ-6438 and GSK126, are currently in the early stages of clinical evaluation and the first encouraging signs of efficacy have recently emerged in the clinic. To anticipate mechanisms of resistance to EZH2i, we used a forward genetic platform combining a...
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