Targeting EZH2 in cancer

Citation metadata

Date: Feb. 2016
From: Nature Medicine(Vol. 22, Issue 2)
Publisher: Nature Publishing Group
Document Type: Report
Length: 6,770 words
Lexile Measure: 1440L

Document controls

Main content

Abstract :

Recent genomic studies have resulted in an emerging understanding of the role of chromatin regulators in the development of cancer. EZH2, a histone methyl transferase subunit of a Polycomb repressor complex, is recurrently mutated in several forms of cancer and is highly expressed in numerous others. Notably, both gain-of-function and loss-of-function mutations occur in cancers but are associated with distinct cancer types. Here we review the spectrum of EZH2-associated mutations, discuss the mechanisms underlying EZH2 function, and synthesize a unifying perspective that the promotion of cancer arises from disruption of the role of EZH2 as a master regulator of transcription. We further discuss EZH2 inhibitors that are now showing early signs of promise in clinical trials and also additional strategies to combat roles of EZH2 in cancer.

Source Citation

Source Citation   

Gale Document Number: GALE|A443459291