title: History of the G protein-coupled receptor (GPCR) assays from traditional to a state-of-the-art biosensor assay.
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.
authors.affiliation: Division of Cancer Pathophysiology, National Cancer Center Research Institute, Japan.
authors.forename: Kanako
authors.initials: K
authors.lastname: Miyano
authors.forename: Yuka
authors.initials: Y
authors.lastname: Sudo
authors.forename: Akinobu
authors.initials: A
authors.lastname: Yokoyama
authors.forename: Kazue
authors.initials: K
authors.lastname: Hisaoka-Nakashima
authors.forename: Norimitsu
authors.initials: N
authors.lastname: Morioka
authors.forename: Minoru
authors.initials: M
authors.lastname: Takebayashi
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Nakata
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Higami
authors.forename: Yasuhito
authors.initials: Y
authors.lastname: Uezono
mesh_terms: D000818:Animals; D015374:Biosensing Techniques / Q000379:methods* / Q000639:trends; D002478:Cells, Cultured; D058266:Dielectric Spectroscopy; D006801:Humans; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000032:analysis* / Q000502:physiology; D015398:Signal Transduction / Q000235:genetics / Q000502:physiology; D014407:Tumor Cells, Cultured
chemical_list: D043562:Receptors, G-Protein-Coupled