Open AccessA Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists
Author(s) -
Ke Liu,
Noel Southall,
Steven A. Titus,
James Inglese,
Robert L. Eskay,
Paul Shinn,
Christopher P. Austin,
Markus Heilig,
Wei Zheng
Publication year - 2010
Publication title -
assay and drug development technologies
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.402
H-Index - 56
eISSN - 1557-8127
pISSN - 1540-658X
DOI - 10.1089/adt.2009.0245
Subject(s) - g protein coupled receptor , multiplex , calcium in biology , receptor , agonist , intracellular , antagonist , calcium , chemistry , fluorescence , high throughput screening , biophysics , microbiology and biotechnology , biochemistry , biology , bioinformatics , physics , organic chemistry , quantum mechanics
Activation of G(q) protein-coupled receptors can be monitored by measuring the increase in intracellular calcium with fluorescent dyes. Recent advances in fluorescent kinetic plate readers and liquid-handling technology have made it possible to follow these transient changes in intracellular calcium in a 1,536-well plate format for high-throughput screening (HTS). Here, we have applied the latest generation of fluorescence kinetic plate readers to multiplex the agonist and antagonist screens of a G protein-coupled receptor (GPCR). This multiplexed assay format provides an efficient and cost-effective method for HTS of G(q)-coupled GPCR targets.