Abstract
Proteolysis-targeting chimeras (PROTACs) have received much attention for their promising therapeutic intervention in recent years. These molecules, with the mechanism of simultaneous recruitment of target protein and an E3 ligase, can trigger the cellular ubiquitin–proteasome system to degrade the target proteins. This article systematically introduces the mechanism of small-molecule PROTACs, and summarized the research progress of small-molecule PROTACs. The prospect for further application and the problems to be solved are also discussed.
Financial & competing interests disclosure
This work was supported by National Natural Science Funds of China [81803372], Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province [2019E10021] and Health Commission of Zhejiang Province [XKQ-010-001, WJK-ZJ-1918]. The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript.
No writing assistance was utilized in the production of this manuscript.