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Current Pharmaceutical Biotechnology


ISSN (Print): 1389-2010
ISSN (Online): 1873-4316

Deciphering G Protein-Coupled Receptor Biology with Fluorescence-based Methods

Author(s): Francisco Ciruela, Antoni Vallano, Maria L. Cuffi, Lourdes Carbonell, Silvia Sanchez, Josep M. Arnau, Carla Tasca, Victor Fernandez-Duenas and Maricel Gomez-Soler

Volume 15, Issue 10, 2014

Page: [962 - 970] Pages: 9

DOI: 10.2174/1389201015666140909125119

Price: $65


G-protein-coupled receptors (GPCRs) represent the main family of cell surface receptors and are virtually expressed in all eukaryotic cells. Interestingly, a large number of clinically used drugs exert their pharmacological effect via a GPCR, thus it seems crucial to deeply understand the biology of these receptors. The study of GPCR activation and signaling has been classically performed by physiological, biochemical and pharmacological approaches using radioactivity-based tools. However, apart from the potential hazards of radioisotope handling and environmental burden, these approaches have some technical limitations. Therefore, the development of fluorescence-based techniques in general and fluorescence and bioluminescence resonance energy transfer (FRET and BRET) in particular have revolutionized the way to study GPCR functioning both in vitro and in vivo. Indeed, these techniques allow the characterization and visualization of all the individual GPCR signaling steps (i.e. ligand binding, receptor activation, G-protein coupling, G-protein activation, GPCR desensitization) with high temporal and spatial resolution. Here, we review the use and impact of fluorescent-based methodologies on the deciphering of GPCR biology.

Keywords: BRET, FRET, G protein-coupled receptor, ligand-receptor interaction, protein-protein interaction.

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