Research progress of protein arginine methyltransferase 5 inhibitors
10.11665/j.issn.1000-5048.20210315
- VernacularTitle:蛋白精氨酸甲基转移酶5抑制剂研究进展
- Author:
Kangning ZHAN
1
;
Xu QUAN
;
Zhangjian HUANG
;
Liwen ZHAO
Author Information
1. 中国药科大学新药研究中心
- Publication Type:Journal Article
- Keywords:
PRMT5;
small molecular inhibitors;
epigenetics;
arginine methylation;
antitumor target
- From:
Journal of China Pharmaceutical University
2021;52(3):371-378
- CountryChina
- Language:Chinese
-
Abstract:
Protein arginine methyltransferases, which proceed the post-translational modification of both histones and non-histones, play an important role in many biological pathways. Protein arginine methyltransferase 5 (PRMT5) is a major enzyme responsible for symmetric di-methylation of arginine residues and has been suggested as a potential therapeutic target for tumors.In the past decade,the discovery and development of PRMT5 inhibitors have become one of the most important research fields.This article introduces the structure and biochemical function of PRMT5 and its correlation with cancer reviews, the binding modes and biological data of PRMT5 inhibitors under development, and discusses the clinical application potential of PRMT5 inhibitors in the treatment of cancer.
