泛素连接酶
泛素
蛋白质降解
药物发现
蛋白酶体
蛋白质水解
泛素蛋白连接酶类
计算生物学
生物信息学
化学
生物
细胞生物学
生物化学
酶
基因
作者
Liwen Xia,Wei Liu,Yifu Song,Hai‐Liang Zhu,Yongtao Duan
标识
DOI:10.2174/1568026619666191011162955
摘要
Proteolysis targeting chimeras (PROTACs), as a novel therapeutic modality, play a vital role in drug discovery. Each PROTAC contains three key parts; a protein-of-interest (POI) ligand, a E3 ligase ligand, and a linker. These bifunctional molecules could mediate the degradation of POIs by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation via the ubiquitin proteasome system (UPS). With several advantages over other therapeutic strategies, PROTACs have set off a new upsurge of drug discovery in recent years. ENDTAC, as the development of PROTACs technology, is now receiving more attention. In this review, we aim to summarize the rapid progress from 2018 to 2019 in protein degradation and analyze the challenges and future direction that need to be addressed in order to efficiently develop potent protein degradation technology.
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