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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.
Assay Drug Dev Technol. 2010 Jun;8(3):367-79. doi: 10.1089/adt.2009.0245.

Related scientific material

Authors Title Source
Ke Liu, Noel Southall, Steve A. Titus, James Inglese, Robert L. Eskay, Paul Shinn, Christopher P. Austin, Markus A. Heilig and Wei Zheng A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists Assay Drug Dev Technol. 2010 Jun;8(3):367-79
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