泛素连接酶
蛋白质水解
泛素
蛋白质降解
DNA连接酶
靶蛋白
计算生物学
细胞生物学
癌症治疗
化学
F盒蛋白
生物
生物化学
癌症
DNA
遗传学
酶
基因
作者
Alberto Ocaña,Atanasio Pandiella
标识
DOI:10.1186/s13046-020-01672-1
摘要
Abstract Exploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ligase. The bridging between the protein of interest and the E3 ligase mediated by the PROTAC facilitates ubiquitination of the protein and its proteasomal degradation. In this review we discuss the molecular medicine behind PROTAC mechanism of action, with special emphasis on recent developments and their potential translation to the clinical setting.
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