Xenopus oocyte electrophysiology in GPCR drug discovery.

Kasper B. Hansen, Hans Bräuner-Osborne

Research output: Contribution to journalArticlepeer-review

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
Pages (from-to)343-357
Number of pages15
JournalMethods in molecular biology (Clifton, N.J.)
Volume552
DOIs
StatePublished - 2009

Fingerprint

Dive into the research topics of 'Xenopus oocyte electrophysiology in GPCR drug discovery.'. Together they form a unique fingerprint.

Cite this