Inhibition of the Histone Lysine Methyltransferase EZH2 for the Treatment of Cancer

Author(s):

Sharad K. Verma   Pages 714 - 719 ( 6 )

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.

Keywords:

Chromatin, epigenetics, histone methyltransferases, nucleosome, post-translational modification.

Affiliation:

GlaxoSmithKline Pharmaceuticals, Inc., 1250 South Collegeville Road, Collegeville, PA 19426, USA.

Graphical Abstract:

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