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 | |
| State | Published - May 8 2013 |
| Externally published | Yes |
Publication series
| Name | Methods in Molecular Biology |
|---|---|
| Volume | 995 |
| ISSN (Print) | 1064-3745 |
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Keywords
- Bivalent ligands
- Calcium mobilization
- G-protein-coupled receptor
- GPCR
- Heteromer
- High-throughput screening
- HTS
- Oligomerization
ASJC Scopus subject areas
- Molecular Biology
- Genetics
Cite this
A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers. / Harvey, Jessica H.; Van Rijn, Richard M.; Whistler, Jennifer.
Chemical Neurobiology: Methods and Protocols. 2013. p. 43-54 (Methods in Molecular Biology; Vol. 995).Research output: Chapter in Book/Report/Conference proceeding › Chapter
}
TY - CHAP
T1 - A FLIPR assay for evaluating agonists and antagonists of GPCR heterodimers
AU - Harvey, Jessica H.
AU - Van Rijn, Richard M.
AU - Whistler, Jennifer
PY - 2013/5/8
Y1 - 2013/5/8
N2 - 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.
AB - 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.
KW - Bivalent ligands
KW - Calcium mobilization
KW - G-protein-coupled receptor
KW - GPCR
KW - Heteromer
KW - High-throughput screening
KW - HTS
KW - Oligomerization
UR - http://www.scopus.com/inward/record.url?scp=84877043027&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84877043027&partnerID=8YFLogxK
U2 - 10.1007/978-1-62703-345-9_4
DO - 10.1007/978-1-62703-345-9_4
M3 - Chapter
SN - 9781627033442
T3 - Methods in Molecular Biology
SP - 43
EP - 54
BT - Chemical Neurobiology
ER -