High-content assays for ligand regulation of G-protein-coupled receptors

被引：61

作者：

Milligan, G ^{[1
]}

机构：

[1] Univ Glasgow, Inst Biomed & Life Sci, Div Biochem & Mol Biol, Mol Pharmacol Grp, Glasgow G12 8QQ, Lanark, Scotland

来源：

DRUG DISCOVERY TODAY | 2003年 / 8卷 / 13期

关键词：

RESONANCE ENERGY-TRANSFER; GREEN FLUORESCENT PROTEIN; CONSTITUTIVELY ACTIVE MUTANT; HETEROTRIMERIC G-PROTEINS; GROWTH-FACTOR RECEPTOR; INDUCED UP-REGULATION; LIVING CELLS; HORMONE-RECEPTOR; BETA(2)-ADRENERGIC RECEPTOR; INDEPENDENT DIMERIZATION;

D O I：

10.1016/S1359-6446(03)02738-7

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

High-content assays rely on the imaging of cellular events. They can be used to monitor the activation of G-protein-coupled receptors (or other receptors), their internalization into the cell, or alterations in their amount. In addition, multiplexed assays can provide further information about the characteristics of the receptor. Recent improvements in throughput using high-content screening platforms means that such assays are now an integral element of functional analysis in the drug discovery process.

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页码：579 / 585

页数：7

相关论文

共 60 条

[1] A pH-sensitive fluor, CypHer™ 5, used to monitor agonist-induced g protein-coupled receptor internalization in live cells [J].

Adie, EJ ;

Kalinka, S ;

Smith, L ;

Francis, MJ ;

Marenghi, A ;

Cooper, ME ;

Briggs, M ;

Michael, NP ;

Milligan, G ;

Game, S .

BIOTECHNIQUES, 2002, 33 (05) :1152-1157

[2]

ADIE EJ, IN PRESS ASSAYS DRUG

[3] Dimerization: An emerging concept for G protein-coupled receptor ontogeny and function [J].

Angers, S ;

Salahpour, A ;

Bouvier, M .

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 2002, 42 :409-435

[4] Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer [J].

Ayoub, MA ;

Couturier, C ;

Lucas-Meunier, E ;

Angers, S ;

Fossier, P ;

Bouvier, M ;

Jockers, R .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (24) :21522-21528

[5] Ligand-independent dimerization of CXCR4, a principal HIV-1 coreceptor [J].

Babcock, GJ ;

Farzan, M ;

Sodroski, J .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2003, 278 (05) :3378-3385

[6] How accurately can we image inositol lipids in living cells? [J].

Balla, T ;

Bondeva, T ;

Várnai, P .

TRENDS IN PHARMACOLOGICAL SCIENCES, 2000, 21 (07) :238-241

[7] Internal trafficking and surface mobility of a functionally intact beta(2)-adrenergic receptor-green fluorescent protein conjugate [J].

Barak, LS ;

Ferguson, SSG ;

Zhang, J ;

Martenson, C ;

Meyer, T ;

Caron, MG .

MOLECULAR PHARMACOLOGY, 1997, 51 (02) :177-184

[8] A beta-arrestin green fluorescent protein biosensor for detecting G protein-coupled receptor activation [J].

Barak, LS ;

Ferguson, SSG ;

Zhang, J ;

Caron, MG .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1997, 272 (44) :27497-27500

[9]

BERGLUND MM, IN PRESS J PHARM EXP

[10] The BRET2/arrestin assay in stable recombinant cells:: A platform to screen for compounds that interact with G protein-coupled receptors (GPCRS) [J].

Bertrand, L ;

Parent, S ;

Caron, M ;

Legault, M ;

Joly, E ;

Angers, S ;

Bouvier, M ;

Brown, M ;

Houle, B ;

Ménard, L .

JOURNAL OF RECEPTOR AND SIGNAL TRANSDUCTION RESEARCH, 2002, 22 (1-4) :533-541

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