AUTHOR=Qi Si-Min , Dong Jinyun , Xu Zhi-Yuan , Cheng Xiang-Dong , Zhang Wei-Dong , Qin Jiang-Jiang 

TITLE=PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

JOURNAL=Frontiers in Pharmacology

VOLUME=12

YEAR=2021

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.692574

DOI=10.3389/fphar.2021.692574

ISSN=1663-9812

ABSTRACT=<p>Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein degradation tool developed in recent years that can ubiquitinate the target proteins through the ubiquitin-proteasome system (UPS) to achieve an effect on tumor growth. A number of literature studies on PROTAC technology have proved an insight into the feasibility of PROTAC technology to degrade target proteins. Additionally, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging results in clinical trials for prostate and breast cancer treatment, which inspires a greater enthusiasm for PROTAC research. Here we focus on the structures and mechanisms of PROTACs and describe several classes of effective PROTAC degraders based on E3 ligases.</p>