Functional assays for screening GPCR targets

被引：173

作者：

Thomsen, W ^{[1
]}

Frazer, J ^{[1
]}

Unett, D ^{[1
]}

机构：

[1] Arena Pharmaceut Inc, San Diego, CA 92121 USA

来源：

CURRENT OPINION IN BIOTECHNOLOGY | 2005年 / 16卷 / 06期

关键词：

D O I：

10.1016/j.copbio.2005.10.008

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

dG-protein-coupled receptors (GPCRs) are valuable molecular targets for drug discovery. An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates. Several functional assay kits based on fluorescence and/or chemiluminescence detection are commercially available for convenient screen development, each having advantages and disadvantages. In addition, new GPCR biosensors and high-content imaging technologies have recently been developed that hold promise for the development of functional GPCR screens in living cells.

引用

收藏

页码：655 / 665

页数：11

相关论文

共 66 条

[1] A fluorescence resonance energy transfer-based sensor indicates that receptor access to a G protein is unrestricted in a living mammalian cell [J].

Azpiazu, I ;

Gautam, N .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (26) :27709-27718

[2]

Behan D P, 2001, Curr Opin Drug Discov Devel, V4, P548

[3] GPCR interacting proteins (GIP) [J].

Bockaert, J ;

Fagni, L ;

Dumuis, A ;

Marin, P .

PHARMACOLOGY & THERAPEUTICS, 2004, 103 (03) :203-221

[4] High-content screening assay for activators of the Wnt/Fzd pathway in primary human cells [J].

Borchert, KM ;

Galvin, RJS ;

Frolik, CA ;

Hale, LV ;

Halladay, DL ;

Gonyier, RJ ;

Trask, OJ ;

Nickischer, DR ;

Houck, KA .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2005, 3 (02) :133-141

[5] Scintillation proximity assay of inositol phosphates in cell extracts: High-throughput measurement of G-protein-coupled receptor activation [J].

Brandish, PE ;

Hill, LA ;

Zheng, W ;

Scolnick, EM .

ANALYTICAL BIOCHEMISTRY, 2003, 313 (02) :311-318

[6] Identification of signal transduction pathways used by orphan G protein-coupled receptors [J].

Bresnick, JN ;

Skynner, HA ;

Chapman, KL ;

Jack, AD ;

Zamiara, E ;

Negulescu, P ;

Beaumont, K ;

Patel, S ;

McAllister, G .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2003, 1 (02) :239-249

[7] Insights into G protein structure, function, and regulation [J].

Cabrera-Vera, TM ;

Vanhauwe, J ;

Thomas, TO ;

Medkova, M ;

Preininger, A ;

Mazzoni, MR ;

Hamm, HE .

ENDOCRINE REVIEWS, 2003, 24 (06) :765-781

[8]

Chambers C, 2003, COMB CHEM HIGH T SCR, V6, P355

[9] A G protein-coupled receptor for UDP-glucose [J].

Chambers, JK ;

Macdonald, LE ;

Sarau, HM ;

Ames, RS ;

Freeman, K ;

Foley, JJ ;

Zhu, Y ;

McLaughlin, MM ;

Murdock, P ;

McMillan, L ;

Trill, J ;

Swift, A ;

Aiyar, N ;

Taylor, P ;

Vawter, L ;

Naheed, S ;

Szekeres, P ;

Hervieu, G ;

Scott, C ;

Watson, JM ;

Murphy, AJ ;

Duzic, E ;

Klein, C ;

Bergsma, DJ ;

Wilson, S ;

Livi, GP .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (15) :10767-10771

[10] Monitoring agonist-promoted conformational changes of β-arrestin in living cells by intramolecular BRET [J].

Charest, PG ;

Terrillon, S ;

Bouvier, M .

EMBO REPORTS, 2005, 6 (04) :334-340

← 1 2 3 4 5 6 7 →