The development of small-molecule inhibitors that target PRC2-related proteins
10.16438/j.0513-4870.2020-0049
- VernacularTitle:靶向PRC2相关蛋白小分子抑制剂的研究进展
- Author:
Jing GU
1
,
2
;
Xiao-ke GUO
1
,
2
;
Qi-dong YOU
1
,
2
Author Information
1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 211198, China
2. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
- Publication Type:Research Article
- Keywords:
epigenetic;
polycomb repressive complex 2;
inhibitor;
protein-protein interaction;
anti-tumor
- From:
Acta Pharmaceutica Sinica
2020;55(8):1726-1734
- CountryChina
- Language:Chinese
-
Abstract:
Abnormal expression of polycomb repressive complex 2 (PRC2) is related to the development of a variety of diseases. Inhibition of normal or overactive PRC2 can reduce cell survival and inhibit tumor growth in several cancers. Therefore, the identification and development of small molecule inhibitors has become an active field of current epigenetic-related anti-tumor strategies. A small molecule inhibitor targeting the S-adenosyl-L-methionine (SAM) binding site of enhancer of zeste homologue 2 (EZH2) has been approved by FDA. However, acquired drug resistance is of concern. Drugs targeting two different binding sites of embryonic ectoderm development (EED) are also being developed. The development of EZH2-EED proton pump inhibitor has attracted extensive attention due to its unique mechanism of action. In this paper, we review the research progress on various small molecule inhibitors that target PRC2-related proteins to provide a basis for further research and development of related drugs.
