Tools for GPCR drug discovery

doi:10.1038/aps.2011.173

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 国家新药筛选中心

	Tools for GPCR drug discovery
	Zhang, Ru 1; Xie, Xin1,2
刊名	ACTA PHARMACOLOGICA SINICA
	2012-03
卷号	33 期号:3 页码:372-384
关键词	G-protein-coupled receptors (GPCRs) high-throughput screening high-content screening functional assay G-protein-dependent assay G-protein-independent assay label-free assay functional selectivity
ISSN号	1671-4083
DOI	10.1038/aps.2011.173
文献子类	Review
英文摘要	G-protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic targets for a broad spectrum of diseases. The design and implementation of high-throughput GPCR assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates are critical in early drug discovery. Early functional GPCR assays depend primarily on the measurement of G-protein-mediated 2nd messenger generation. Taking advantage of the continuously deepening understanding of GPCR signal transduction, many G-protein-independent pathways are utilized to detect the activity of GPCRs, and may provide additional information on functional selectivity of candidate compounds. With the combination of automated imaging systems and label-free detection systems, such assays are now suitable for high-throughput screening (HTS). In this review, we summarize the most widely used GPCR assays and recent advances in HTS technologies for GPCR drug discovery.
资助项目	Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2008DFB30150] ; National Natural Science Foundation of China[31071227] ; National Natural Science Foundation of China[90713047] ; Shanghai Commission of Science and Technology[09DZ2260100]
WOS关键词	PROTEIN-COUPLED-RECEPTORS ; TIME-RESOLVED FRET ; CELLULAR DIELECTRIC-SPECTROSCOPY ; ENZYME FRAGMENT COMPLEMENTATION ; BETA-ARRESTIN RECRUITMENT ; SNAP-TAG TECHNOLOGIES ; GTP-BINDING ASSAY ; CRYSTAL-STRUCTURE ; 7-TRANSMEMBRANE RECEPTORS ; INTRACELLULAR CALCIUM
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000301187300010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278168]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Xie, Xin
作者单位	1.Tongji Univ, Shanghai Key Lab Signaling & Dis Res, Lab Receptor Based Biomed, Sch Life Sci & Technol, Shanghai 200092, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Ru,Xie, Xin. Tools for GPCR drug discovery[J]. ACTA PHARMACOLOGICA SINICA,2012,33(3):372-384.
APA	Zhang, Ru,&Xie, Xin.(2012).Tools for GPCR drug discovery.ACTA PHARMACOLOGICA SINICA,33(3),372-384.
MLA	Zhang, Ru,et al."Tools for GPCR drug discovery".ACTA PHARMACOLOGICA SINICA 33.3(2012):372-384.