组蛋白甲基化转移酶 - 一个有吸引力的抗癌靶点

Title:G9a - An Appealing Antineoplastic Target

Volume: 17 Issue: 6

关键词: 组蛋白赖氨酸甲基化转移酶，组蛋白甲基化转移酶G9a，生物功能抑制剂，疾病，肿瘤靶点。

摘要: 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.

Cite this article as:

G9a - An Appealing Antineoplastic Target, Current Cancer Drug Targets 2017; 17 (6) . https://dx.doi.org/10.2174/1568009616666160512145303

DOI https://dx.doi.org/10.2174/1568009616666160512145303	Print ISSN 1568-0096
Publisher Name Bentham Science Publisher	Online ISSN 1873-5576