Deciphering G Protein-Coupled Receptor Biology with Fluorescence-based Methods
2014
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.
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