Xenopus oocyte electrophysiology in GPCR drug discovery

Kasper Bø Hansen, Hans Bräuner-Osborne

    11 Citations (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.
    Original languageEnglish
    Title of host publicationG protein-coupled receptors in drug discovery
    EditorsWayne R Leifert
    Volume552
    Place of PublicationUnited States
    PublisherHumana Press
    Publication date2009
    Pages343-357
    ISBN (Print)978-1-60327-316-9
    ISBN (Electronic)978-1-60327-317-6
    DOIs
    Publication statusPublished - 2009
    SeriesMethods in Molecular Biology
    Volume552
    ISSN1064-3745

    Keywords

    • Former Faculty of Pharmaceutical Sciences

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