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

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

Volume: 15 Issue: 8

Author(s): Sharad K. Verma

Affiliation:

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.

Cite this article as:

Verma K. Sharad, Inhibition of the Histone Lysine Methyltransferase EZH2 for the Treatment of Cancer, Current Topics in Medicinal Chemistry 2015; 15 (8) . https://dx.doi.org/10.2174/1568026615666150302105207