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

Author(s): Sharad K. Verma

Journal Name: Current Topics in Medicinal Chemistry

Volume 15 , Issue 8 , 2015

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Graphical 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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Article Details

Year: 2015
Published on: 12 March, 2015
Page: [714 - 719]
Pages: 6
DOI: 10.2174/1568026615666150302105207
Price: $65

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