Abstract:
: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.
journal_name
J Pharmacol Scijournal_title
Journal of pharmacological sciencesauthors
Miyano K,Sudo Y,Yokoyama A,Hisaoka-Nakashima K,Morioka N,Takebayashi M,Nakata Y,Higami Y,Uezono Ydoi
10.1254/jphs.14R13CPsubject
Has Abstractpub_date
2014-01-01 00:00:00pages
302-9issue
4eissn
1347-8613issn
1347-8648pii
DN/JST.JSTAGE/jphs/14R13CPjournal_volume
126pub_type
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