Monitoring Gq-coupled receptor response through inositol phosphate quantification with the IP-One assay.

Trinquet E, Bouhelal R, Dietz M


Cisbio Bioassays, Codolet, France. Novartis Pharma AG, F. Hoffmann LaRoche AG

Expert Opin. Drug Discov. (2011);6(10):981-994.

G-protein-coupled receptors (GPCRs) are transmembrane proteins that play a key role in the signal transduction of extracellular stimuli. GPCRs associate to a complex assembly of intracellular proteins regulating a large variety of signaling pathways. In particular, the production of inositol 1,4,5 triphosphate (IP3) signs the activation of Gq-coupled receptors. However, its very short half-life makes its assessment too challenging for drug screening operations and the monitoring of calcium release, triggered by IP3, has been extensively used as a downstream readout of this signaling pathway. Recently, a new homogeneous time-resolved fluorescence (HTRF) assay, detecting a downstream metabolite of IP3, inositol monophosphate (IP1), has overcome the drawbacks of the IP3 quantification, allowing its use in primary or secondary screening.

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IP-One Gq assay kits