Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay.

Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay. Research Abstract Details 

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Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay. Abstract Text:

The measurement of ligand receptor binding parameters for G-protein-coupled receptors is indispensable in the drug discovery process. Traditional ligand receptor binding assays require scale-up of cells and membrane preparations, which is an expensive and time-consuming process. In this report, the authors describe the development of a homogeneous live-cell binding assay for GPCRs using a fluorophore-labeled nonpeptide ligand. The model assay used Cy3B-labeled telenzepine and Chinese hamster ovary cells expressing M1 muscarinic acetylcholine receptors. This homogeneous live-cell fluorescence binding assay format is superior to the traditional binding methods because it measures binding of a ligand to intact receptors on living cells. The assay requires no washing or separation steps, thereby allowing a real-time kinetic readout for the determination of ligand association and dissociation from the intact receptors. The results also suggest that miniaturization is feasible without compromising the data quality. ( Journal of Biomolecular Screening 2008:748-754).

Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay. Publishing Authors By Initials

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Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Journal of biomolecular screening : the official j

VOLUME: 13

Page Numbers: 748-54

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ISSN: 1087-0571

DAY: 6

MONTH: 05

YEAR: 2008

Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Development of a homogeneous high-throughput live-cell g-protein-coupled receptor binding assay.

AFFILIATION: Chemistry Research and Discovery, Amgen, Inc., Thousand Oaks, California. paull@amgen.com.

Country: United States

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MEDLINETA: J Biomol Screen

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