ArticleMolecular pharmacology2011
G protein-coupled receptor heteromerization: a role in allosteric modulation of ligand binding.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 55 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
55 citing papers in PubMed, 86 citations in OpenAlex.
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- Unlocking opioid neuropeptide dynamics with genetically encoded biosensors.Nature neuroscience · 2024Article
- Cannabidiol at Nanomolar Concentrations Negatively Affects Signaling through the Adenosine AInternational journal of molecular sciences · 2023Article
- Peptidomimetics and Their Applications for Opioid Peptide Drug Discovery.Biomolecules · 2022Review
- Challenges and new opportunities for detecting endogenous opioid peptides in reward.Addiction neuroscience · 2022Article
- Compartment-specific opioid receptor signaling is selectively modulated by different dynorphin peptides.eLife · 2021Article
- The Balance of MU-Opioid, Dopamine D2 and Adenosine A2A Heteroreceptor Complexes in the Ventral Striatal-Pallidal GABA Antireward Neurons May Have a Significant Role in Morphine and Cocaine Use Disorders.Frontiers in pharmacology · 2021Article
- Five Decades of Research on Opioid Peptides: Current Knowledge and Unanswered Questions.Molecular pharmacology · 2020Review
- Biased signaling by endogenous opioid peptides.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Mu Opioid Receptor Heterodimers Emerge as Novel Therapeutic Targets: Recent Progress and Future Perspective.Frontiers in pharmacology · 2020Review
- New Insights on Expression and Function of Mu and Delta Opioid Receptors in Mouse Gastrointestinal Tract.Cellular and molecular gastroenterology and hepatology · 2020Article
- Mu and Delta Opioid Receptors Are Coexpressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon.Cellular and molecular gastroenterology and hepatology · 2020Article
- Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation.Neurogastroenterology and motility · 2019Article
- The Endocannabinoid System as a Target in Cancer Diseases: Are We There Yet?Frontiers in pharmacology · 2019Review
- Regulation of an Opioid Receptor Chaperone Protein, RTP4, by Morphine.Molecular pharmacology · 2019Article
- Dynamic lateral organization of opioid receptors (kappa, muTraffic (Copenhagen, Denmark) · 2018Article
- Heteromerization of μ-opioid receptor and cholecystokinin B receptor through the third transmembrane domain of the μ-opioid receptor contributes to the anti-opioid effects of cholecystokinin octapeptide.Experimental & molecular medicine · 2018Article
- Heteromerization Modulates mu Opioid Receptor Functional PropertiesFrontiers in pharmacology · 2018Review
- Two delta opioid receptor subtypes are functional in single ventral tegmental area neurons, and can interact with the mu opioid receptor.Neuropharmacology · 2017Article
- The opioid receptor triple agonist DPI-125 produces analgesia with less respiratory depression and reduced abuse liability.Acta pharmacologica Sinica · 2017Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
It is becoming increasingly recognized that G protein-coupled receptors physically interact. These interactions may provide a mechanism for allosteric modulation of receptor function. In this study, we examined this possibility by using an established model system of a receptor heteromer consisting of μ and δ opioid receptors. We examined the effect of a number of μ receptor ligands on the binding equilibrium and association and dissociation kinetics of a radiolabeled δ receptor agonist, [(3)H]deltorphin II. We also examined the effect of δ receptor ligands on the binding equilibrium and association and dissociation kinetics of a radiolabeled μ receptor agonist, [(3)H][d-Ala(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin ([(3)H]DAMGO). We show that μ receptor ligands are capable of allosterically enhancing δ receptor radioligand binding and vice versa. Thus, there is strong positive cooperativity between the two receptor units with remarkable consequences for ligand pharmacology. We find that the data can be simulated by adapting an allosteric receptor model previously developed for small molecules, suggesting that the ligand-occupied protomers function as allosteric modulators of the partner receptor's activity.
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Registered trials
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.