Xenopus oocyte electrophysiology in GPCR drug discovery
Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research
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 language | English |
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Title of host publication | G protein-coupled receptors in drug discovery |
Editors | Wayne R Leifert |
Volume | 552 |
Place of Publication | United States |
Publisher | Humana Press |
Publication date | 2009 |
Pages | 343-357 |
ISBN (Print) | 978-1-60327-316-9 |
ISBN (Electronic) | 978-1-60327-317-6 |
DOIs | |
Publication status | Published - 2009 |
Series | Methods in Molecular Biology |
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Volume | 552 |
ISSN | 1064-3745 |
Bibliographical note
Keywords: Xenopus laevis, Oocyte, RNA, Transcription, Injection, GPRC6A, Intracellular calcium, Ligand.
Chapter 25
- Former Faculty of Pharmaceutical Sciences
Research areas
ID: 13063250