GPCR screening via ERK 1/2: a novel platform for screening G protein-coupled receptors
| Autor: | Cheryl Turner, Andrea Brown, Ronald Ian William Osmond, Emma Barnett, Georgina Harvey, Michael Francis Crouch, Romana Borowicz, Antony James Sheehan, Anthony Ross Dyer |
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| Rok vydání: | 2005 |
| Předmět: |
MAPK/ERK pathway
Mitogen-Activated Protein Kinase 3 Biology Transfection Biochemistry Analytical Chemistry Cell Line Receptors G-Protein-Coupled chemistry.chemical_compound Chlorocebus aethiops Animals Humans Cyclic adenosine monophosphate Receptor Neurotensin G protein-coupled receptor Mitogen-Activated Protein Kinase 1 COS cells Cell biology chemistry Mitogen-activated protein kinase COS Cells biology.protein Molecular Medicine Phosphorylation Carbachol Biotechnology |
| Zdroj: | Journal of biomolecular screening. 10(7) |
| ISSN: | 1087-0571 |
| Popis: | Discovery of novel agonists and antagonists for G protein-coupled receptors (GPCRs) relies heavily on cell-based assays because determination of functional consequences of receptor engagement is often desirable. Currently, there are several key parameters measured to achieve this, including mobilization of intracellular Ca2+ and formation of cyclic adenosine monophosphate or inositol triphosphate. However, no single assay platform is suitable for all situations, and all of the assays have limitations. The authors have developed a new high-throughput homogeneous assay platform for GPCR discovery as an alternative to current assays, which employs detection of phosphorylation of the key signaling molecule p42/44 MAP kinase (ERK 1/2). The authors show that ERK 1/2 is consistently activated in cells stimulated by Gq-coupled GPCRs and provides a new high-throughput platform for screening GPCR drug candidates. The activation of ERK 1/2 in Gq-coupled GPCR systems generates comparable pharmacological data for receptor agonist and antagonist data obtained by other GPCR activation measurement techniques. |
| Databáze: | OpenAIRE |
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