History of the G protein-coupled receptor (GPCR) assays from traditional to a state-of-the-art biosensor assay

The g protein-coupled receptors (gpcrs) form the largest and the most versatile superfamily that share a seven-transmembrane-spanning architecture. gpcr-signaling is involved in vision,taste,olfaction,sympathetic/parasympathetic nervous functions,metabolism,and immune regulation,indicating that gpcrs are extremely important therapeutic targets for various diseases. cellular dielectric spectroscopy (cds) is a novel technology that employs a label-free,real-time and cell-based assay approach for the comprehensive pharmacological evaluation of cells that exogenously or endogenously express gpcrs. among the biosensors that use cds technology,the cellkey™ system not only detects the activation of gpcrs but also distinguishes between signals through different subtypes of the gα protein (gs,gi/o,and gq). in this review,we discuss the traditional assays and then introduce the principles by which the cellkey™ system evaluates gpcr activation,followed by a perspective on the advantages and future prospects of this system. © the japanese pharmacological society.