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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

Author(s): Sharad K. Verma

Volume 15, Issue 8, 2015

Page: [714 - 719] Pages: 6

DOI: 10.2174/1568026615666150302105207

Price: $65

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.

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