HTS Instrument Discovers Low Affinity Inhibitors of the Inositol Phosphate IP Signaling Pathway

Dell EJ, Orban M, Tardieu JL, Degorce F


BMG LABTECH GmbH, Ortenberg, Germany. Cisbio Bioassays, Codolet, France

5th HTRF Symposium, Avignon, France

G-protein coupled receptors (GPCRs are transmembrane proteins which play a key role in the signal transduction of extracellular stimuli. GPCRs are associated with a complex assembly of intracellular proteins regulating a large variety of downstream effectors. The production of inositol 1,4,5-triphosphate (IP3) is one such second messenger, which is produced in response to the activation of Gq-coupled receptors. However, IP3’s very short half-life make its assessment too challenging for drug screening assays and the monitoring of calcium release, triggered by IP3, has been extensively used as a downstream readout of this signaling pathway.

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