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

Literature Life Science

An overview of the use of the IP1 assay in screening processes, with highlights on the discrimination of slow acting compounds and the characterization of inverse agonists


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.


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

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