Portraying G protein-coupled receptors with fluorescent ligands.

ABSTRACT: The thermodynamics of ligand-receptor interactions at the surface of living cells represents a fundamental aspect of G protein-coupled receptor (GPCR) biology; thus, its detailed elucidation constitutes a challenge for modern pharmacology. Interestingly, fluorescent ligands have been developed for a variety of GPCRs in order to monitor ligand-receptor binding in living cells. Accordingly, new methodological strategies derived from noninvasive fluorescence-based approaches, especially fluorescence resonance energy transfer (FRET), have been successfully developed to characterize ligand-receptor interactions. Importantly, these technologies are supplanting more hazardous and expensive radioactive binding assays. In addition, FRET-based tools have also become extremely powerful approaches for

SUBMITTER: Ciruela F 

PROVIDER: S-EPMC4168789 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature