The histone lysine methyltransferase EZH2 is the catalytic component of the multi-protein PRC2 complex and methylates lysine 27 on histone H3. EZH2 overexpression is implicated in tumorigenesis and correlates with poor prognosis in several tumor types. Inhibition of aberrant EZH2 activity might attenuate tumorigenesis resulting from misregulated gene transcription derived from aberrant EZH2 activity. In the last year, the first reports of small molecules demonstrating potent and selective inhibition of EZH2 have been published by multiple groups. Herein, we review recent progress reported in the discovery of small molecule inhibitors of EZH2.
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