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GPCR Screening via ERK 1/2: A Novel Platform for Screening G Protein-Coupled Receptors
From TGR BioSciences Pty Ltd, Thebarton, Australia.
* To whom correspondence should be addressed. E-mail: michael.crouch{at}tgr-biosciences.com.au.
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. Key Words: ERK 1/2, GPCR, cell-based assay, HTS, MAPK
First published on August 29, 2005, doi:10.1177/1087057105277968 This article has been cited by other articles:
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