Journal of Pharmacological Sciences
Online ISSN : 1347-8648
Print ISSN : 1347-8613
ISSN-L : 1347-8613
Current Perspective
History of the G Protein–Coupled Receptor (GPCR) Assays From Traditional to a State-of-the-Art Biosensor Assay
Kanako MiyanoYuka SudoAkinobu YokoyamaKazue Hisaoka-NakashimaNorimitsu MoriokaMinoru TakebayashiYoshihiro NakataYoshikazu HigamiYasuhito Uezono
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2014 Volume 126 Issue 4 Pages 302-309


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 CellKeyTM 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 CellKeyTM system evaluates GPCR activation, followed by a perspective on the advantages and future prospects of this system.

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© 2014 The Japanese Pharmacological Society
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