Research progress in controllable proteolysis targeting chimeras
10.16438/j.0513-4870.2023-0553
- VernacularTitle:可控性蛋白降解靶向嵌合体 (PROTACs) 技术研究进展
- Author:
Yi MOU
1
,
2
;
Shuai WEN
1
,
2
;
Yan WANG
1
,
2
;
Zheng-yu JIANG
3
Author Information
1. College of Pharmacy and Chemistry &
2. Chemical Engineering, Taizhou University, Taizhou 225300, China
3. Jiangsu Key Laboratory of Drug Design and Optimization, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
- Publication Type:Research Article
- Keywords:
proteolysis targeting chimeras;
targeted protein degradation;
controllable proteolysis targeting chimeras
- From:
Acta Pharmaceutica Sinica
2023;58(8):2193-2202
- CountryChina
- Language:Chinese
-
Abstract:
Proteolysis targeting chimeras (PROTACs) is an innovative technique in targeted protein degradation. PROTACs is a heterobifunctional molecule which can bind to the E3 ligase and target protein to form a ubiquitination complex, resulting in the ubiquitin-proteasome system dependent degradation of target protein. PROTACs has been regarded as the promising method in drug discovery campaign, for its high commonality, potent degradation activity and unique selectivity profile. However, the catalytic mechanism also induces the uncontrollable protein degradation risk. Controllable PROTACs contain the responsive element in the molecular entity. In certain conditions, the element can be triggered to activate or terminate the degradation event. In this review, we will briefly summarize the strategies in controllable PROTACs and describe the representative examples according to the responsive mechanism. We hope this review could provide some insight into the further development of controllable PROTACs.
