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绑定还是不绑定:解开 G 蛋白偶联受体的多效性之谜。

To Bind or Not to Bind: Unravelling GPCR Polypharmacology.

机构信息

Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville VIC 3052, Australia; School of Pharmacy, Fudan University, Shanghai 201203, China.

Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville VIC 3052, Australia.

出版信息

Cell. 2018 Feb 8;172(4):636-638. doi: 10.1016/j.cell.2018.01.018.

Abstract

Interaction of a single drug with multiple targets through "polypharmacology" is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.

摘要

通过“多药理学”,一种药物与多个靶点相互作用,对于治疗精神分裂症等复杂疾病变得越来越重要。G 蛋白偶联受体(GPCR)是主要的药物靶点,了解 GPCR 药物选择性和混杂性的结构基础,可以为药物开发提供新途径。

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