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DiscoveRx Expands its GPCR Technology Portfolio to Include Advanced Technologies

Published: Friday, April 09, 2010
Last Updated: Friday, April 09, 2010
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Introduces two additional GPCR platforms to facilitate counterscreening, lead optimization and SAR evaluation of compounds.

DiscoveRx continues to innovate in the field of GPCR signaling assays, tools and services with the introduction of two additional GPCR platforms to facilitate counterscreening, lead optimization and SAR evaluation of compounds identified during a primary screen.

Endocytosis is fundamental to GPCR biology, regulating the amount of cell-surface receptors, helping to transduce signals from the receptor and controlling the recycling or degradation of the receptor itself. Therefore, quantitative analysis of the internalization kinetics of the receptor from the cell surface can lead to the discovery of novel compounds with unique attributes.

The PathHunter™ Activated GPCR Internalization technology is a non-imaging, non-antibody based platform that provides a direct and quantitative measurement of internalized GPCR localized to intracellular endosomes allowing the fate of unlabeled, activated GPCRs to be monitored in live cells. Unlike other traditional internalization technologies, PathHunter™ Assays are simple, non-radioactive chemiluminescent assays that are ideal for studying GPCR receptor recycling and kinetics, determining mechanism of action of lead compounds or identifying novel inhibitors of receptor internalization.

The PathHunter™ ß-Arrestin Ortholog GPCR assays are fully validated, functional clonal cell lines expressing ortholog GPCRs that have been optimized to detect a full range of compound pharmacologies. With a portfolio of more than 80 ortholog GPCR targets, drug discovery researchers can gain a greater understanding of putative leads, determine mechanism of action, or delineate differential ligand-activated responses of lead compounds prior to testing in expensive animal models.

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