Xenopus oocyte electrophysiology in GPCR drug discovery

Kasper Bø Hansen, Hans Bräuner-Osborne

    11 Citationer (Scopus)

    Abstract

    Deorphanization of the large group of G protein-coupled receptors (GPCRs) for which an endogenous activating ligand has not yet been identified (orphan GPCRs) has become increasingly difficult. A specialized technique that has been successfully applied to deorphanize some of these GPCRs involves two-electrode voltage-clamp recordings of currents through ion channels, which are activated by GPCRs heterologously expressed in Xenopus oocytes. The ion channels that couple to GPCR activation in Xenopus oocytes can be endogenous calcium-activated chloride channels (CaCCs) or heterologously expressed G protein-coupled inwardly rectifying potassium channels (GIRKs). We will describe a general approach for expression of GPCRs in Xenopus oocytes and characterization of these using electrophysiological recordings. We will focus on the detection of GPCR activation by recordings of currents through CaCCs that are activated by calcium release from the endoplasmic reticulum and thus the G(q) signaling pathway.
    OriginalsprogEngelsk
    TitelG protein-coupled receptors in drug discovery
    RedaktørerWayne R Leifert
    Vol/bind552
    UdgivelsesstedUnited States
    ForlagHumana Press
    Publikationsdato2009
    Sider343-357
    ISBN (Trykt)978-1-60327-316-9
    ISBN (Elektronisk)978-1-60327-317-6
    DOI
    StatusUdgivet - 2009
    NavnMethods in Molecular Biology
    Vol/bind552
    ISSN1064-3745

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    • Det tidligere Farmaceutiske Fakultet

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