New Findings in Drug-Induced Receptor Activity

A research team led by Dr. Michel Bouvier at the Institute for Research in Immunology and Cancer (IRIC) of the University of Montreal in Quebec, used the Roche xCELLigence SP Instrument to measure changes in cell response following ligand stimulation (Stallaert et al., 2012, PloS ONE 7(1): e29420). According to their findings, selective pharmacological inhibition of specific arms of the β2AR signaling network was able to correlate the differential contribution of signaling events to specific components of the cell response. The essential role of intracellular Ca2+ in the cell response also led to the discovery of a novel β2AR-promoted Ca2+ mobilization event.

The discovery that drugs targeting a single G protein-coupled receptor (GPCR) can differentially modulate distinct subsets of the receptor signaling repertoire is a very important step in drug discovery. Findings of the present study underscore the power of using real-time cell monitoring to dissect the pluridimensionality of GPCR signaling using integrative approaches for a comprehensive readout of drug-induced cellular activity.