EZH2-activating mutation: no reliable indicator for efficacy of methyltransferase inhibitors.

Abstract excerpt

EZH2 gain of function mutations (EZH2GOFmu) has been implicated in the pathogenesis of B-non-Hodgkin lymphoma. The EZH2-specific inhibitor GSK126 inhibits trimethylation of histone H3K27 and induces target gene expression. However, in 3/4 EZH2GOFmu B-NHL lymphoma cell lines, GSK126 (400 nM) did not induce growth arrest. Only at high doses (10 µM), the inhibitor was effective as antiproliferative agent, comparably...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to Cell Line, Tumor
• Share to Enhancer of Zeste Homolog 2 Protein