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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