Current Perspective : History of the G Protein–Coupled Receptor (GPCR) Assays From Traditional to a State-of-the-Art Biosensor Assay History of the G Protein–Coupled Receptor (GPCR) Assays From Traditional to a State-of-the-Art Biosensor Assay
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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<sup>TM</sup> system not only detects the activation of GPCRs but also distinguishes between signals through different subtypes of the G<i>α</i> protein (Gs, Gi/o, and Gq). In this review, we discuss the traditional assays and then introduce the principles by which the CellKey<sup>TM</sup> system evaluates GPCR activation, followed by a perspective on the advantages and future prospects of this system.
- Journal of Pharmacological Sciences
Journal of Pharmacological Sciences 126(4), 302-309, 2014
The Japanese Pharmacological Society