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

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

Volume: 15 Issue: 10

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Ciruela Francisco, Vallano Antoni, Cuffi L. Maria, Carbonell Lourdes, Sanchez Silvia, Arnau M. Josep, Tasca Carla, Fernandez-Duenas Victor and Gomez-Soler Maricel, Deciphering G Protein-Coupled Receptor Biology with Fluorescence-based Methods, Current Pharmaceutical Biotechnology 2014; 15 (10) . https://dx.doi.org/10.2174/1389201015666140909125119