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

Access this Article

Author(s)

    • Sudo Yuka Sudo Yuka
    • Division of Cancer Pathophysiology, National Cancer Center Research Institute, Japan|Department of Molecular Pathology and Metabolic Disease, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan
    • Yokoyama Akinobu [他] Yokoyama Akinobu
    • Division of Cancer Pathophysiology, National Cancer Center Research Institute, Japan|Department of Molecular Pathology and Metabolic Disease, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan
    • Morioka Norimitsu
    • Department of Pharmacology, Hiroshima University Graduate School of Biomedical Sciences, Japan
    • Takebayashi Minoru
    • Division of Psychiatry and Neuroscience, Institute for Clinical Research, Department of Psychiatry, National Hospital Organization (NHO) Kure Medical Center and Chugoku Cancer Center, Japan
    • Nakata Yoshihiro
    • Department of Pharmacology, Hiroshima University Graduate School of Biomedical Sciences, Japan
    • Higami Yoshikazu
    • Department of Molecular Pathology and Metabolic Disease, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan
    • Uezono Yasuhito
    • Division of Cancer Pathophysiology, National Cancer Center Research Institute, Japan

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<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

  • Journal of Pharmacological Sciences

    Journal of Pharmacological Sciences 126(4), 302-309, 2014

    The Japanese Pharmacological Society

Codes

  • NII Article ID (NAID)
    130004704288
  • NII NACSIS-CAT ID (NCID)
    AA11806667
  • Text Lang
    ENG
  • ISSN
    1347-8613
  • NDL Article ID
    026003823
  • NDL Call No.
    Z53-D199
  • Data Source
    NDL  J-STAGE 
Page Top