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Drug Discov Today. 2003 Jul 1;8(13):579-85.

High-content assays for ligand regulation of G-protein-coupled receptors.

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  • 1Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK G12 8QQ.


High-content assays rely on the imaging of cellular events. They can be used to monitor the activation of G-protein-coupled receptors (or other receptors), their internalization into the cell, or alterations in their amount. In addition, multiplexed assays can provide further information about the characteristics of the receptor. Recent improvements in throughput using high-content screening platforms means that such assays are now an integral element of functional analysis in the drug discovery process.

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