G9a - an Appealing Antineoplastic Target.

G9a - an Appealing Antineoplastic Target.

Curr Cancer Drug Targets. 2016 May 12;

Authors: Chen WL, Sun HP, Li DD, Wang ZH, You QD, Guo XK

Abstract
G9a is the primary enzyme for mono- and dimethylation at Lys 9 of histone H3 (H3K9me1 and H3K9me2) and forms predominantly the heteromeric complex as a G9a-GLP (G9a-like protein) that is a functional histone lysine methltransferase in vivo. Mounting evidence suggests that G9a catalyzes methylation of histone and nonhistone proteins, which plays a crucial role in diverse biological processes and human diseases. G9a have attracted great attention of scientists as an appealing antineoplastic target. Here, we review the current knowledge on biological functions of G9a, with particular emphasis on regulating gene expression and cell processes, and involvement in human diseases. We outline a perspective on various classes of G9a inhibitors to date from both articles and patents with an emphasis on their discovery, activity and the current research status. These hold future directions and opportunities for a rapid translation of G9a inhibitors into clinical practice for a number of aggressive cancers and other human diseases.

PMID: 27174055 [PubMed - as supplied by publisher]

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