ArticleFASEB journal : official publication of the Federation of American Societies for Experimental Biology2014
Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism.
Article in FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 50 citations in OpenAlex.
- Characterising C-X-C Chemokine Receptor 4 Dynamics in the Cell Membrane Using Fluorescence Fluctuation Spectroscopy.Biomolecules · 2026Article
- Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine HJournal of medicinal chemistry · 2022Article
- Regionally selective cardiovascular responses to adenosine AFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Acylation of the Incretin Peptide Exendin-4 Directly Impacts Glucagon-Like Peptide-1 Receptor Signaling and Trafficking.Molecular pharmacology · 2021Article
- Efficient G protein coupling is not required for agonist-mediated internalization and membrane reorganization of the adenosine AFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2021Article
- Chemical Probes for the Adenosine Receptors.Pharmaceuticals (Basel, Switzerland) · 2019Review
- Probe dependence of allosteric enhancers on the binding affinity of adenosine ABritish journal of pharmacology · 2019Article
- Development of novel fluorescent histamine HScientific reports · 2018Article
- Real-time analysis of the binding of fluorescent VEGFBiochemical pharmacology · 2017Article
- Protein-ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling.MedChemComm · 2017Review
- Review
- Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the humanPharmacology research & perspectives · 2016Article
- The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors.Biochemical Society transactions · 2016Review
- Basic Pharmacological and Structural Evidence for Class A G-Protein-Coupled Receptor Heteromerization.Frontiers in pharmacology · 2016Review
- Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.Neuropharmacology · 2015Review
- Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2015Article
- Native serotonin 5-HT2C receptors are expressed as homodimers on the apical surface of choroid plexus epithelial cells.Molecular pharmacology · 2015Article
- Investigation of GPCR allosterism and dimerization in single living cells using fluorescent ligands.SpringerPlus · 2015Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
In our previous work, using a fluorescent adenosine-A3 receptor (A3AR) agonist and fluorescence correlation spectroscopy (FCS), we demonstrated high-affinity labeling of the active receptor (R*) conformation. In the current study, we used a fluorescent A3AR antagonist (CA200645) to study the binding characteristics of antagonist-occupied inactive receptor (R) conformations in membrane microdomains of individual cells. FCS analysis of CA200645-occupied A3ARs revealed 2 species, τD2 and τD3, that diffused at 2.29 ± 0.35 and 0.09 ± 0.03 μm(2)/s, respectively. FCS analysis of a green fluorescent protein (GFP)-tagged A3AR exhibited a single diffusing species (0.105 μm(2)/s). The binding of CA200645 to τD3 was antagonized by nanomolar concentrations of the A3 antagonist MRS 1220, but not by the agonist NECA (up to 300 nM), consistent with labeling of R. CA200645 normally dissociated slowly from the A3AR, but inclusion of xanthine amine congener (XAC) or VUF 5455 during washout markedly accelerated the reduction in the number of particles exhibiting τD3 characteristics. It is notable that this effect was accompanied by a significant increase in the number of particles with τD2 diffusion. These data show that FCS analysis of ligand-occupied receptors provides a unique means of monitoring ligand A3AR residence times that are significantly reduced as a consequence of allosteric interaction across the dimer interface
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