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PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy.

ABSTRACT: 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.

SUBMITTER: Qi SM

PROVIDER: S-EPMC8138175 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature

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PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy.

Qi Si-Min SM Dong Jinyun J Xu Zhi-Yuan ZY Cheng Xiang-Dong XD Zhang Wei-Dong WD Qin Jiang-Jiang JJ

Frontiers in pharmacology 20210507

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 clinica ...[more]

PMID: 34025443

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