期刊
FUTURE MEDICINAL CHEMISTRY
卷 11, 期 20, 页码 2715-2734出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0161
关键词
degrader; E3 ligases; induced protein degradation; PROTACs; small molecules; ubiquitinproteasome system
资金
- National Natural Science Funds of China [81803372]
- Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province [2019E10021]
- Health Commission of Zhejiang Province [XKQ-010-001, WJK-ZJ-1918]
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.
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