Title:Inhibition of the Histone Lysine Methyltransferase EZH2 for the Treatment of Cancer
VOLUME: 15 ISSUE: 8
Author(s):Sharad K. Verma
Affiliation:GlaxoSmithKline Pharmaceuticals, Inc., 1250 South Collegeville Road, Collegeville, PA 19426, USA.
Keywords:Chromatin, epigenetics, histone methyltransferases, nucleosome, post-translational modification.
Abstract:In recent years, there has been an increased effort in the development of therapies which
target an epigenetic mode of action. Among thes e efforts include progress in the development of inhibitors
of EZH2 (Enhancer of Zeste Homolog 2), a key epigenetic target with strong disease implications
to cancer. Over the last 3+ years, multiple reports describing small molecule inhibitors of EZH2
have been described, including those for chemical probes and drug candidates which have entered the
clinic as first-in-class agents. Recent progress in this emerging area is presented in this review.
