Inhibition of the histone lysine methyltransferase EZH2 for the treatment of cancer

Research output: Contribution to journalArticle


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.

Original languageEnglish (US)
Pages (from-to)714-719
Number of pages6
JournalCurrent Topics in Medicinal Chemistry
Issue number8
Publication statusPublished - 2015
Externally publishedYes



  • Chromatin
  • Epigenetics
  • Histone methyltransferases
  • Nucleosome
  • Post-translational modification

ASJC Scopus subject areas

  • Drug Discovery

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