Recent advances in small molecule PROTACs for the treatment of cancer.

Recent advances in small molecule PROTACs for the treatment of cancer. Curr Med Chem. 2020 Nov 17;: Authors: Li W, Elhassan RM, Hou X, Fang H Abstract The PROTAC (PROteolysis TArgeting Chimera) technology is a target protein degradation strategy, based on the ubiquitin-proteasome system, which has been gradually developed into a potential means of targeted cancer therapy in recent years. This strategy has already shown significant advantages over traditional small-molecule inhibitors in terms of pharmacodynamics, selectivity, and drug resistance. Several small molecule PROTACs have been in a Phase I clinical trial. Herein, we introduced the mechanism, characteristics, and advantages of PROTAC strategy. And we summarize the recent advances in the development of small-molecule PROTACs for cancer treatment. We hope this review will be helpful in optimizing the design of the ideal small-molecule PROTACs and advancing targeted anticancer research. PMID: 33208057 [PubMed - as supplied by publisher]
Source: Current Medicinal Chemistry - Category: Chemistry Authors: Tags: Curr Med Chem Source Type: research