title: A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers.
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.
authors.affiliation: Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA, USA.
authors.forename: Jessica H
authors.initials: JH
authors.lastname: Harvey
authors.forename: Richard M
authors.initials: RM
authors.lastname: van Rijn
authors.forename: Jennifer L
authors.initials: JL
authors.lastname: Whistler
mesh_terms: D001597:Benzylidene Compounds / Q000494:pharmacology*; D020013:Calcium Signaling; D018929:Cell Culture Techniques; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000494:pharmacology*; D057809:HEK293 Cells; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D017465:Receptors, Opioid, delta / Q000819:agonists* / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D011994:Recombinant Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D013050:Spectrometry, Fluorescence; D014162:Transfection
chemical_list: D001597:Benzylidene Compounds; D043562:Receptors, G-Protein-Coupled; D017465:Receptors, Opioid, delta; D011994:Recombinant Proteins; C077358:7-benzylidenenaltrexone; D009271:Naltrexone; D020881:Enkephalin, D-Penicillamine (2,5)-