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Journal of Biomolecular Screening, Vol. 13, No. 5, 424-429 (2008)
DOI: 10.1177/1087057108318332

Cell-Free Assay of G-Protein-Coupled Receptors Using Fluorescence Polarization

Jessi Wildeson Jones

Biologics and Biomolecular Sciences, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut

Tiffani A. Greene

Integral Molecular, Inc., Philadelphia, Pennsylvania

Christine A. Grygon

Biologics and Biomolecular Sciences, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut

Benjamin J. Doranz

Integral Molecular, Inc., Philadelphia, Pennsylvania

Martha P. Brown

Biologics and Biomolecular Sciences, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut, martha.brown{at}boehringer-ingelheim.com

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 EC50 determined for the CXCR4-T-22 peptide interaction via FP with CXCR4 lipoparticles (15 nM) is consistent with the IC50 determined for the unlabeled T-22 peptide via competitive binding (59 nM). (Journal of Biomolecular Screening 2008:424-429)

Key Words: nanotechnology • lipoparticle • fluorescence polarization • GPCR


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