可药性
蛋白酶体
蛋白质降解
蛋白质水解
药物发现
泛素
计算生物学
生物
生物信息学
细胞生物学
生物化学
酶
基因
作者
Nuwayo Ishimwe Sincere,Krishnan Anand,Sumel Ashique,Jing Yang,Chongge You
出处
期刊:Molecules
[Multidisciplinary Digital Publishing Institute]
日期:2023-05-10
卷期号:28 (10): 4014-4014
被引量:88
标识
DOI:10.3390/molecules28104014
摘要
A potential therapeutic strategy to treat conditions brought on by the aberrant production of a disease-causing protein is emerging for targeted protein breakdown using the PROTACs technology. Few medications now in use are tiny, component-based and utilize occupancy-driven pharmacology (MOA), which inhibits protein function for a short period of time to temporarily alter it. By utilizing an event-driven MOA, the proteolysis-targeting chimeras (PROTACs) technology introduces a revolutionary tactic. Small-molecule-based heterobifunctional PROTACs hijack the ubiquitin-proteasome system to trigger the degradation of the target protein. The main challenge PROTAC's development facing now is to find potent, tissue- and cell-specific PROTAC compounds with favorable drug-likeness and standard safety measures. The ways to increase the efficacy and selectivity of PROTACs are the main focus of this review. In this review, we have highlighted the most important discoveries related to the degradation of proteins by PROTACs, new targeted approaches to boost proteolysis' effectiveness and development, and promising future directions in medicine.
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