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Portraying G Protein-Coupled Receptors with Fluorescent Ligands
- Source :
- ACS Chemical Biology
- Publication Year :
- 2014
- Publisher :
- American Chemical Society (ACS), 2014.
-
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 visualizing receptor-receptor interactions (i.e., GPCR oligomerization) in living cells. Thus, by means of the synthesis of compatible fluorescent ligands these novel techniques can be implemented to demonstrate the existence of GPCR oligomerization not only in heterologous systems but also in native tissues. Finally, there is no doubt that these methodologies would also be relevant in drug discovery in order to develop new high-throughput screening approaches or to identify new therapeutic targets. Overall, herein, we provide a thorough assessment of all technical and biological aspects, including strengths and weaknesses, of these fluorescence-based methodologies when applied to the study of GPCR biology at the plasma membrane of living cells.
- Subjects :
- Drug discovery
Cell Membrane
Reviews
General Medicine
Biology
Ligands
Biochemistry
Fluorescence
Receptors, G-Protein-Coupled
Cell biology
Förster resonance energy transfer
Drug Discovery
Fluorescence Resonance Energy Transfer
Biophysics
Humans
Molecular Medicine
Fluorescent Dyes
G protein-coupled receptor
Subjects
Details
- ISSN :
- 15548937 and 15548929
- Volume :
- 9
- Database :
- OpenAIRE
- Journal :
- ACS Chemical Biology
- Accession number :
- edsair.doi.dedup.....fd0af26acf7961d8e9dc2447272559b2