蛋白质降解
泛素
蛋白酶体
蛋白质水解
药物发现
计算生物学
机制(生物学)
生物
生物信息学
细胞生物学
生物化学
酶
基因
认识论
哲学
作者
Stacey-Lynn Paiva,Craig M. Crews
标识
DOI:10.1016/j.cbpa.2019.02.022
摘要
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the degradation of select proteins of interest (POIs) by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation by the 26S proteasome. This hijacking mechanism has been used to degrade various types of disease-relevant POIs. In this review, we aim to highlight the recent advances in targeted protein degradation and describe the challenges that need to be addressed in order to efficiently develop potent PROTACs.
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