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Portraying G Protein-Coupled Receptors with Fluorescent Ligands
[Image: see text] 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 be...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2014
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168789/ https://www.ncbi.nlm.nih.gov/pubmed/25010291 http://dx.doi.org/10.1021/cb5004042 |
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author | Ciruela, Francisco Jacobson, Kenneth A. Fernández-Dueñas, Víctor |
author_facet | Ciruela, Francisco Jacobson, Kenneth A. Fernández-Dueñas, Víctor |
author_sort | Ciruela, Francisco |
collection | PubMed |
description | [Image: see text] 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. |
format | Online Article Text |
id | pubmed-4168789 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | American Chemical
Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-41687892015-07-10 Portraying G Protein-Coupled Receptors with Fluorescent Ligands Ciruela, Francisco Jacobson, Kenneth A. Fernández-Dueñas, Víctor ACS Chem Biol [Image: see text] 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. American Chemical Society 2014-07-10 2014-09-19 /pmc/articles/PMC4168789/ /pubmed/25010291 http://dx.doi.org/10.1021/cb5004042 Text en Copyright © 2014 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) |
spellingShingle | Ciruela, Francisco Jacobson, Kenneth A. Fernández-Dueñas, Víctor Portraying G Protein-Coupled Receptors with Fluorescent Ligands |
title | Portraying G Protein-Coupled Receptors with Fluorescent
Ligands |
title_full | Portraying G Protein-Coupled Receptors with Fluorescent
Ligands |
title_fullStr | Portraying G Protein-Coupled Receptors with Fluorescent
Ligands |
title_full_unstemmed | Portraying G Protein-Coupled Receptors with Fluorescent
Ligands |
title_short | Portraying G Protein-Coupled Receptors with Fluorescent
Ligands |
title_sort | portraying g protein-coupled receptors with fluorescent
ligands |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168789/ https://www.ncbi.nlm.nih.gov/pubmed/25010291 http://dx.doi.org/10.1021/cb5004042 |
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