Enhanced performance of the new HTRF® cAMP kit on Gài/o coupled GPCR

L. Affleck, S. Bdioui, S. Junique, N. Douayry, S. Soldevila, E. Bourrier, T. Roux, E. Trinquet. Cisbio, Cisbio, Codolet, France.

G-protein-coupled receptors (GPCR) are cell surface receptors which remain a major class of target in the drug discovery process. The assessment of the Gi/o pathway relies on the detection of cyclic AMP, which is one of the most important GPCR intracellular mediators. Gi/o coupled activation receptors lead to the inhibition of cAMP production in cells. This assay accurately detects the decrease in intracellular cAMP concentration upon GPCR activation. In this context, we are introducing a new HTRF® assay to specifically investigate the Gi/o pathway and to accurately characterize agonist and antagonist compounds. Thereby, the addition of this new HTRF Gi assay to existing HTRF® Gs and Gq assays means the establishment of a powerful platform dedicated to the identification and the characterization of compounds against GPCR.