Back to Search
Start Over
Cell-Free Assay of G-Protein-Coupled Receptors Using Fluorescence Polarization
- Source :
- SLAS Discovery: Advancing Life Sciences R&D; June 2008, Vol. 13 Issue: 5 p424-429, 6p
- Publication Year :
- 2008
-
Abstract
- A recently developed nanotechnology, the Integral Molecular lipoparticle, provides an essentially soluble cell-free system in which G-protein-coupled receptors (GPCRs) in their native conformations are concentrated within virus-like particles. As a result, the lipoparticle provides a means to overcome 2 common obstacles to the development of homogeneous, nonradioactive GPCR ligand-binding assays: membrane protein solubilization and low receptor density. The work reported here describes the first application of this nanotechnology to a fluorescence polarization (FP) molecular binding assay format. The GPCR chosen for these studies was the well-studied chemokine receptor CXCR4 for which a peptide ligand (T-22) has been previously characterized. The EC50determined for the CXCR4-T-22 peptide interaction via FP with CXCR4 lipoparticles (15 nM) is consistent with the IC50determined for the unlabeled T-22 peptide via competitive binding (59 nM).
Details
- Language :
- English
- ISSN :
- 24725552 and 24725560
- Volume :
- 13
- Issue :
- 5
- Database :
- Supplemental Index
- Journal :
- SLAS Discovery: Advancing Life Sciences R&D
- Publication Type :
- Periodical
- Accession number :
- ejs59508678
- Full Text :
- https://doi.org/10.1177/1087057108318332