Recent progress in the discovery of small-molecule inhibitors of the HMT EZH2 for the treatment of cancer

Sharad K. Verma, Steven D. Knight

Research output: Contribution to journalReview article

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1661-1670
Number of pages10
JournalFuture medicinal chemistry
Volume5
Issue number14
DOIs
StatePublished - Sep 1 2013

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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