ArticleFrontiers in molecular neuroscience2019
GRK Mediates μ-Opioid Receptor Plasma Membrane Reorganization.
Article in Frontiers in molecular neuroscience, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 21 citations in OpenAlex.
- Characterising C-X-C Chemokine Receptor 4 Dynamics in the Cell Membrane Using Fluorescence Fluctuation Spectroscopy.Biomolecules · 2026Article
- Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail.CNS drugs · 2025Review
- Key phosphorylation sites for robust β-arrestin2 binding at the MOR revisited.Communications biology · 2024Article
- Ligand-Directed Labeling of the Adenosine AJournal of medicinal chemistry · 2024Article
- Selective targeting of mu opioid receptors to primary cilia.Cell reports · 2024Article
- Review
- Unraveling the hidden temporal range of fast βCommunications biology · 2022Article
- Signaling-Biased and Constitutively Active Dopamine D2 Receptor Variant.ACS chemical neuroscience · 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
- Review
- Opioid Pharmacology under the Microscope.Molecular pharmacology · 2020Review
- Single-molecule analysis reveals agonist-specific dimer formation of µ-opioid receptors.Nature chemical biology · 2020Article
- Post-translational Modifications of Opioid Receptors.Trends in neurosciences · 2020Review
- Homologous Regulation of Mu Opioid Receptor Recycling by GMolecular pharmacology · 2019Article
- Ligand-dependent spatiotemporal signaling profiles of the μ-opioid receptor are controlled by distinct protein-interaction networks.The Journal of biological chemistry · 2019Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylation, desensitization, plasma membrane redistribution, and internalization. Here, we used fluorescence correlation spectroscopy (FCS) and fluorescence recovery after photobleaching (FRAP) to detect and quantify ligand-dependent changes in the plasma membrane organization of MOP expressed in human embryonic kidney (HEK293) cells. The low internalizing agonist morphine and the antagonist naloxone did not alter constitutive MOP plasma membrane organization. In contrast, the internalizing agonist DAMGO changed MOP plasma membrane organization in a pertussis toxin-insensitive manner and by two mechanisms. Firstly, it slowed MOP diffusion in a manner that was independent of internalization but dependent on GRK2/3. Secondly, DAMGO reduced the surface receptor number and the proportion of mobile receptors, and increased receptor clustering in a manner that was dependent on clathrin-mediated endocytosis. Overall, these results suggest the existence of distinct sequential MOP reorganization events at the plasma membrane and provide insights into the specific protein interactions that control MOP plasma membrane organization.
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Registered trials
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