靶向G蛋白偶联受体高通量药物筛选技术研究进展  

Advance in high-throughput drug screening techniques targeting G protein-coupled receptors

作　　者：杨秀颖[1] 张莉[1] 杜冠华[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所药物靶点研究与新药筛选北京市重点实验室,北京100050

出　　处：《中国新药杂志》2012年第22期2636-2641,共6页Chinese Journal of New Drugs

基　　金：国家科技部魁北克国际合作项目(2008DFA31710);国家"重大新药创制"科技重大专项(2009ZX09302-003;2009ZX09102-123);国家自然科学基金(81102492)

摘　　要：G蛋白偶联受体(GPCR)是临床广泛应用药物的主要靶点之一。靶向GPCR的高通量药物筛选新技术不断涌现,为发现高效、高选择性、低毒的药物提供可能,并使选择合理的GPCR药物筛选策略显得尤为重要。本文综述了靶向GPCR药物高通量筛选相关技术及策略的研究进展,主要包括基于GPCR受体配体结合、第二信使、β-arrestin、调控元件报告基因、内化、聚合体及变构调节剂等方面的高通量药物筛选技术,以及相关技术的代表性商品化产品以供参考。G protein-coupled receptors （GPCRs） are important drug targets, which have been widely used in clinical practice. New assay techniques for high-throughput screening of drugs targeting GPCRs are emerging in large numbers nowadays, providing the possibility to discover the more efficient, higher selective, lower toxic GPCR drugs. The techniques make the rational design and implementation for GPCR drug screening particularly important. In this paper, we reviewed the progress of techniques and strategies for high-throughput screening of drugs targeting GPCRs, mainly including the strategies on receptor-ligand binding, second messenger detection, β- arrestin, reporter gene, internalization, oligomerizations and allosteric modulators. We also summarized some of the representative commercial techniques for reference.

关 键 词：G蛋白偶联受体 高通量药物筛选 药物发现 

分 类 号：R965.1[医药卫生—药理学]