G9a - An Appealing Antineoplastic Target

Author(s): Wei-Lin Chen, Hao-Peng Sun, Dong-Dong Li, Zhi-Hui Wang, Qi-Dong You*, Xiao-Ke Guo*

Journal Name: Current Cancer Drug Targets

Volume 17 , Issue 6 , 2017

  Journal Home
Translate in Chinese
Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Background: G9a is the primary enzyme for mono- and dimethylation at Lys 9 of histone H3 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.

Methods: In this study, the current knowledge on biological functions of G9a and inhibitors were summarized.

Results: 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.

Conclusion: We highlight the key knowledge on potential biological functions and various human diseases. We also reviewed the discovery and characterization of the reported G9a inhibitors. However, we also propose the challenges and future opportunities in study of G9a. This review could make a crucial contribution to the long journey to develop drug-like molecules targeting G9a.

Keywords: Histone Lysine Methltransferase, G9a, Biological functions, inhibitors, diseases, antineoplastic target.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2017
Published on: 29 June, 2017
Page: [555 - 568]
Pages: 14
DOI: 10.2174/1568009616666160512145303
Price: $65

Article Metrics

PDF: 64