A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists | Zendy

Ke Liu | Zendy; Noel Southall | Zendy; Steve A. Titus | Zendy; James Inglese | Zendy; Robert L. Eskay | Zendy; Paul Shinn | Zendy; Christopher P. Austin | Zendy; Markus Heilig | Zendy; Wei Zheng | Zendy

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A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists

Author(s) -

Ke Liu,

Noel Southall,

Steve 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.

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