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Methods Mol Biol. 2013;995:43-54. doi: 10.1007/978-1-62703-345-9_4.

A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers.

Author information

1
Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA, USA.

Abstract

Calcium signaling plays a major role in the function of cells. Measurement of intracellular calcium mobilization is a robust assay that can be performed in a high-throughput manner to study the effect of compounds on potential drug targets. Pharmaceutical companies frequently use calcium signaling assays to screen compound libraries on G-protein-coupled receptors (GPCRs). In this chapter we describe the application of FLIPR technology to the evaluation of GPCR-induced calcium mobilization. We also include the implications of GPCR hetero-oligomerization and the identification of heteromeric receptors as novel drug targets on high-throughput calcium screening.

PMID:
23494371
PMCID:
PMC6428067
DOI:
10.1007/978-1-62703-345-9_4
[Indexed for MEDLINE]
Free PMC Article

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