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Journal of Biomolecular Screening
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Article

Development of a Homogeneous High-Throughput Live-Cell G-Protein-Coupled Receptor Binding Assay

Paul H. Lee*, Steven C. Miller, Carlo van Staden, and Evan F. Cromwell

Amgen Inc.

* To whom correspondence should be addressed. E-mail: paull{at}amgen.com.


  Abstract
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 XXXX:xx-xx)

First published on May 6, 2008, doi:10.1177/1087057108317835

Journal of Biomolecular Screening 2008;13:748.

A more recent version of this article appeared on September 1, 2008

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