Tools for GPCR drug discovery
文献类型：期刊论文
| 作者 | Zhang, Ru1; Xie, Xin1,2
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 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. |
| 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 |
| 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研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000301187300010 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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