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 proceedingChapter

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 languageEnglish (US)
Title of host publicationChemical Neurobiology
Subtitle of host publicationMethods and Protocols
Pages43-54
Number of pages12
DOIs
StatePublished - May 8 2013
Externally publishedYes

Publication series

NameMethods in Molecular Biology
Volume995
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

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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