自噬
蛋白质降解
蛋白酶体
泛素
计算生物学
脱氮酶
生物信息学
生物
细胞生物学
生物化学
基因
细胞凋亡
作者
Jin Li,Xinxin Chen,Aiping Lü,Chao Liang
出处
期刊:The Innovation
[Elsevier BV]
日期:2023-03-15
卷期号:4 (3): 100413-100413
被引量:32
标识
DOI:10.1016/j.xinn.2023.100413
摘要
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology can be used to target proteins by hijacking the ubiquitin-proteasome system. Conceptually, PROTAC aims to target the "undruggable" majority of proteins in the human proteome. Through constant exploration and optimization of PROTACs and the exploitation of other TPD strategies over two decades, TPD has expanded from theoretical studies to clinical strategies, with practical applications in oncological, immunological, and other diseases. In this review, we introduce the mechanisms, features, and molecular targets of orthodox PROTACs and summarize the PROTAC drugs under study as cancer therapeutics in clinical trials. We also discuss PROTAC derivatives and other TPD strategies, such as lysosome-targeting chimeras, autophagy-targeting chimeras, and molecular glue strategies. Collectively, the studies summarized herein support the full potential of TPD in the biomedical industry.
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