High-Throughput Fluorescence Assays for Ion Channels and GPCRs

Irina Vetter; David Carter; John Bassett; Jennifer R Deuis; Bryan Tay; Sina Jami; Samuel D Robinson

doi:10.1007/978-3-030-12457-1_3

High-Throughput Fluorescence Assays for Ion Channels and GPCRs

Adv Exp Med Biol. 2020:1131:27-72. doi: 10.1007/978-3-030-12457-1_3.

Authors

Irina Vetter^{1

2}, David Carter³, John Bassett⁴, Jennifer R Deuis³, Bryan Tay³, Sina Jami³, Samuel D Robinson³

Affiliations

¹ Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD, Australia. i.vetter@uq.edu.au.
² School of Pharmacy, The University of Queensland, St. Lucia, QLD, Australia. i.vetter@uq.edu.au.
³ Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD, Australia.
⁴ School of Pharmacy, The University of Queensland, St. Lucia, QLD, Australia.

PMID: 31646506
DOI: 10.1007/978-3-030-12457-1_3

Abstract

Ca²⁺, Na⁺ and K⁺- permeable ion channels as well as GPCRs linked to Ca²⁺ release are important drug targets. Accordingly, high-throughput fluorescence plate reader assays have contributed substantially to drug discovery efforts and pharmacological characterization of these receptors and ion channels. This chapter describes some of the basic properties of the fluorescent dyes facilitating these assay approaches as well as general methods for establishment and optimisation of fluorescence assays for ion channels and G_q-coupled GPCRs.

Keywords: Assay development; FLIPR; Fluorescence imaging; G protein-coupled receptor; High-content; High-throughput; Ligand-gated ion channel; Optimization; Voltage-gated ion channel.

Publication types

Review

MeSH terms

Animals
Biological Assay* / trends
Drug Discovery
Fluorescent Dyes / metabolism
Humans
Ion Channels* / analysis
Receptors, G-Protein-Coupled* / analysis

Substances

Fluorescent Dyes
Ion Channels
Receptors, G-Protein-Coupled