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Journal of Biomolecular Screening
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GPCR Screening via ERK 1/2: A Novel Platform for Screening G Protein–Coupled Receptors

Ronald I. W. Osmond

Antony Sheehan

Romana Borowicz

Emma Barnett

Georgina Harvey

Cheryl Turner

Andrea Brown

Michael F. Crouch

TGR BioSciences Pty Ltd, 31 Dalgleish Street, Thebarton, SA 5031 Australiamichael.crouch{at}tgr-biosciences.com.au

Anthony R. Dyer

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

This version was published on October 1, 2005

Journal of Biomolecular Screening, Vol. 10, No. 7, 730-737 (2005)
DOI: 10.1177/1087057105277968
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[Abstract] [PDF]