ArticleJournal of neurochemistry2012
Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R.
Article in Journal of neurochemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed.
- Fluorescent APurinergic signalling · 2023Article
- Exploring the Effect of Halogenation in a Series of Potent and Selective AJournal of medicinal chemistry · 2023Article
- Overcoming the Challenges of Detecting GPCR Oligomerization in the Brain.Current neuropharmacology · 2022Article
- Molecular probes for the human adenosine receptors.Purinergic signalling · 2021Review
- Allosteric Interactions between Adenosine AInternational journal of molecular sciences · 2021Review
- Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization.Methods in cell biology · 2021Review
- Design, Synthesis and Characterization of a New Series of Fluorescent Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulators.Molecules (Basel, Switzerland) · 2020Article
- Adenosine ACells · 2019Article
- Chemical Probes for the Adenosine Receptors.Pharmaceuticals (Basel, Switzerland) · 2019Review
- Functional and Neuroprotective Role of Striatal Adenosine AJournal of caffeine and adenosine research · 2019Review
- Effects of Long-Term Alcohol Drinking on the Dopamine D2 Receptor: Gene Expression and Heteroreceptor Complexes in the Striatum in Rats.Alcoholism, clinical and experimental research · 2018Article
- Mapping the Interface of a GPCR Dimer: A Structural Model of the AFrontiers in pharmacology · 2018Article
- The D2 Dopamine Receptor Interferes With the Protective Effect of the AFrontiers in neuroscience · 2018Article
- Synthesis and Characterization of a New Bivalent Ligand Combining Caffeine and Docosahexaenoic Acid.Molecules (Basel, Switzerland) · 2017Article
- Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding.British journal of pharmacology · 2016Review
- New paradigms in GPCR drug discovery.Biochemical pharmacology · 2015Review
- Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.Neuropharmacology · 2015Review
- Application of BRET to monitor ligand binding to GPCRs.Nature methods · 2015Article
- Untangling dopamine-adenosine receptor-receptor assembly in experimental parkinsonism in rats.Disease models & mechanisms · 2015Article
- Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism.ACS chemical biology · 2014Article
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Authors and funding
7 authors.
Funding
Abstract
In the CNS, an antagonistic interaction has been shown between adenosine A(2A) and dopamine D(2) receptors (A(2A)Rs and D(2)Rs) that may be relevant both in normal and pathological conditions (i.e., Parkinson's disease). Thus, the molecular determinants mediating this receptor-receptor interaction have recently been explored, as the fine tuning of this target (namely the A(2A)R/D(2)R oligomer) could possibly improve the treatment of certain CNS diseases. Here, we used a fluorescence resonance energy transfer-based approach to examine the allosteric modulation of the D(2)R within the A(2A)R/D(2)R oligomer and the dependence of this receptor-receptor interaction on two regions rich in positive charges on intracellular loop 3 of the D(2)R. Interestingly, we observed a negative allosteric effect of the D(2)R agonist quinpirole on A(2A)R ligand binding and activation. However, these allosteric effects were abolished upon mutation of specific arginine residues (217-222 and 267-269) on intracellular loop 3 of the D(2)R, thus demonstrating a major role of these positively charged residues in mediating the observed receptor-receptor interaction. Overall, these results provide structural insights to better understand the functioning of the A(2A)R/D(2)R oligomer in living cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.