靶向G蛋白偶联受体的高通量药物筛选方法  

High-throughput screening assays for G-protein-coupled receptors-targeted drug discovery

作　　者：李静[1] 谢欣[1] 

机构地区：[1]中国科学院上海药物研究所,上海201203

出　　处：《国际药学研究杂志》2012年第5期353-357,共5页Journal of International Pharmaceutical Research

基　　金：国家自然科学基金项目(81202341);上海市优秀学术带头人(12XD1402100);上海市科学技术委员会科技计划项目(11DZ2292200)

摘　　要：G蛋白偶联受体(G-protein-coupled receptors,GPCR)是一类具有7次跨膜结构的膜蛋白。GPCR介导多种重要的生理功能,与很多疾病密切相关,是最重要的现代药物靶点家族。目前市场上有近50%的药物是以GPCR为靶点的。因此,GPCR分析方法和GPCR配体筛选方法的研究是当今世界新药研究的重点和热点。本文归纳介绍了近年来被广泛使用的GPCR药物发现方法,以及靶向GPCR高通量筛选技术的最新研究进展。Gproteincoupled receptors （ GPCR）, also known as 7 transmembrane receptors, are the largest family of cell sur face receptors. GPCR mediate many important physiological functions and are among the most successful therapeutic targets for a broad spectrum of diseases. These receptors are the targets of 〉 50% of the current therapeutic agents on the market. Therefore, GPCR assay development and GPCR ligand screening remain the major focus of drug discovery research worldwide. In this review, we summarize the most widely used GPCR assays and recent advances in highthroughput screening technology for GPCR drug discovery.

关 键 词：G蛋白偶联受体 信号转导 药物发现 高通量筛选 

分 类 号：R965.1[医药卫生—药理学]