Inhibition of the histone lysine methyltransferase EZH2 for the treatment of cancer.
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.
GlaxoSmithKline Pharmaceuticals, Inc., 1250 South Collegeville Road, Collegeville, PA 19426, USA. sharad.k.verma@gsk.com.
Sharad K
SK
Verma
D000970:Antineoplastic Agents / Q000494:pharmacology*; D000071221:Enhancer of Zeste Homolog 2 Protein; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D044127:Epigenesis, Genetic; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D063151:Polycomb Repressive Complex 2 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; C498409:EZH2 protein, human; D000071221:Enhancer of Zeste Homolog 2 Protein; D063151:Polycomb Repressive Complex 2