TY - JOUR
T1 - The use of Xenopus oocytes in drug screening
AU - Kvist, Trine
AU - Hansen, Kasper Bø
AU - Bräuner-Osborne, Hans
N1 - Keywords: drug discovery, drug screening, electrophysiology, GPCR, ligand-gated ion channel, transporter, two-electrode voltage-clamp, voltage-gated ion channel, Xenopus oocytes
PY - 2011/2
Y1 - 2011/2
N2 - Introduction: The physiological roles of ion channels are receiving increased interest in both basic research and drug discovery, and a demand for pharmacological approaches that can characterize or screen ion channels and their ligands with higher throughput has emerged. Traditionally, screening of compound libraries at ion channel targets has been performed using assays such as binding assays, fluorescence-based assays and flux assays that allow high-throughput, but sacrifice high data quality. The use of these assays with ion channel targets can also be problematic, emphasizing the usefulness of automated Xenopus oocyte electrophysiological assays in drug screening. Areas covered: This review summarizes the use of Xenopus oocytes in drug screening, presents the advantages and disadvantages of the use of Xenopus oocytes as expression system, and addresses the options available for automated two-electrode voltage-clamp recordings from Xenopus oocytes. Expert opinion: Automated and manual Xenopus oocyte two-electrode voltage-clamp recordings are useful and important techniques in drug screening. Although they are not compatible with high-throughput experimentation, these techniques are excellent in combination or as alternatives to fluorescence-based assays for hit validation, screening of focused compound libraries and safety screening on ion channels with their high flexibility for the choice of molecular targets, quality of data and reproducibility.
AB - Introduction: The physiological roles of ion channels are receiving increased interest in both basic research and drug discovery, and a demand for pharmacological approaches that can characterize or screen ion channels and their ligands with higher throughput has emerged. Traditionally, screening of compound libraries at ion channel targets has been performed using assays such as binding assays, fluorescence-based assays and flux assays that allow high-throughput, but sacrifice high data quality. The use of these assays with ion channel targets can also be problematic, emphasizing the usefulness of automated Xenopus oocyte electrophysiological assays in drug screening. Areas covered: This review summarizes the use of Xenopus oocytes in drug screening, presents the advantages and disadvantages of the use of Xenopus oocytes as expression system, and addresses the options available for automated two-electrode voltage-clamp recordings from Xenopus oocytes. Expert opinion: Automated and manual Xenopus oocyte two-electrode voltage-clamp recordings are useful and important techniques in drug screening. Although they are not compatible with high-throughput experimentation, these techniques are excellent in combination or as alternatives to fluorescence-based assays for hit validation, screening of focused compound libraries and safety screening on ion channels with their high flexibility for the choice of molecular targets, quality of data and reproducibility.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1517/17460441.2011.546396
DO - 10.1517/17460441.2011.546396
M3 - Review
C2 - 22647133
SN - 1746-0441
VL - 6
SP - 141
EP - 153
JO - Expert Opinion on Drug Discovery
JF - Expert Opinion on Drug Discovery
IS - 2
ER -