A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers

Jessica H. Harvey; Richard M. Van Rijn; Jennifer Whistler

doi:10.1007/978-1-62703-345-9_4

A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers

Jessica H. Harvey, Richard M. Van Rijn, Jennifer Whistler

Research output: Chapter in Book/Report/Conference proceeding › Chapter

2 Scopus citations

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.

Original language	English (US)
Title of host publication	Chemical Neurobiology
Subtitle of host publication	Methods and Protocols
Pages	43-54
Number of pages	12
DOIs	https://doi.org/10.1007/978-1-62703-345-9_4
State	Published - May 8 2013
Externally published	Yes

Publication series

Name	Methods in Molecular Biology
Volume	995
ISSN (Print)	1064-3745

Keywords

Bivalent ligands
Calcium mobilization
G-protein-coupled receptor
GPCR
Heteromer
High-throughput screening
HTS
Oligomerization

ASJC Scopus subject areas

Molecular Biology
Genetics

Access to Document

10.1007/978-1-62703-345-9_4

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Cite this

Harvey, J. H., Van Rijn, R. M., & Whistler, J. (2013). A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers. In Chemical Neurobiology: Methods and Protocols (pp. 43-54). (Methods in Molecular Biology; Vol. 995). https://doi.org/10.1007/978-1-62703-345-9_4

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