Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery

[Display omitted] Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin–proteasome system (UPS) to induce different POIs degradation. Currently, the first ora...

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Bibliographic Details
Published in:Bioorganic chemistry 2022-08, Vol.125, p.105848-105848, Article 105848
Main Authors: Xi, Jia-Yue, Zhang, Ru-Yue, Chen, Ke, Yao, Lin, Li, Mu-Qiong, Jiang, Ru, Li, Xiao-Ye, Fan, Li
Format: Article
Language:English
Subjects:
Drug discovery
PROTACs
Small inhibitors
Target protein degradation
Undruggable target
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Summary:[Display omitted] Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin–proteasome system (UPS) to induce different POIs degradation. Currently, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging efficacy in clinical trials of prostate and breast cancer treatment, which turns a new avenue for the development of PROTAC research. In this review, we focus on a detailed summary of the latest progress of PROTACs and elucidate the advantages of PROTACs technology. In addition, potential challenges and perspectives of PRTOACs are discussed.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2022.105848