Evaluating cellular impedance assays for detection of GPCR pleiotropic signaling and functional selectivity

MF Peters, CW Scott - SLAS Discovery, 2009 - Elsevier
G-protein–coupled receptors can couple to different signal transduction pathways in different
cell types (termed cell-specific signaling) and can activate different signaling pathways
depending on the receptor conformation (s) stabilized by the activating ligand (functional
selectivity). These concepts offer potential for developing pathway-specific drugs that
increase efficacy and reduce side effects. Despite significant interest, functional selectivity
has been difficult to exploit in drug discovery, in part due to the burden of multiple assays …