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How Physiologic Targets Can Be Distinguished from Drug-Binding Proteins
Molecular Pharmacology ( IF 3.6 ) Pub Date : 2021-07-01 , DOI: 10.1124/molpharm.120.000186
Kojo Mensa-Wilmot 1
Affiliation  

In clinical trials, some drugs owe their effectiveness to off-target activity. This and other observations raise a possibility that many studies identifying targets of drugs are incomplete. If off-target proteins are pharmacologically important, it will be worthwhile to identify them early in the development process to gain a better understanding of the molecular basis of drug action. Herein, we outline a multidisciplinary strategy for systematic identification of physiologic targets of drugs in cells. A drug-binding protein whose genetic disruption yields very similar molecular effects as treatment of cells with the drug may be defined as a physiologic target of the drug. For a drug developed with a rational approach, it is desirable to verify experimentally that a protein used for hit optimization in vitro remains the sole polypeptide recognized by the drug in a cell.

中文翻译:

如何区分生理靶点与药物结合蛋白

在临床试验中,一些药物的有效性归功于脱靶活性。这个和其他观察提出了一种可能性,即许多确定药物靶点的研究是不完整的。如果脱靶蛋白在药理学上很重要,那么在开发过程的早期识别它们以更好地了解药物作用的分子基础将是值得的。在这里,我们概述了系统识别细胞中药物生理靶点的多学科策略。其遗传破坏产生与用药物处理细胞非常相似的分子效应的药物结合蛋白可被定义为药物的生理靶标。对于以合理方法开发的药物,
更新日期:2021-07-04
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