ArticleMolecular pharmacology2011
Cholesterol regulates micro-opioid receptor-induced beta-arrestin 2 translocation to membrane lipid rafts.
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 33 papers.
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Who cites it
33 citing papers in PubMed, 49 citations in OpenAlex.
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the µ-opioid receptor.Nature communications · 2026Article
- Location-biased β-arrestin conformations direct GPCR signaling.Science signaling · 2026Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor.bioRxiv : the preprint server for biology · 2025Article
- Selective targeting of mu opioid receptors to primary cilia.Cell reports · 2024Article
- G Protein-Coupled Receptor Dimerization-What Next?International journal of molecular sciences · 2024Review
- Three-Dimensional Structural Insights Have Revealed the Distinct Binding Interactions of Agonists, Partial Agonists, and Antagonists with the µ Opioid Receptor.International journal of molecular sciences · 2023Review
- Patching holes in the mechanism of opioid tolerance.Trends in pharmacological sciences · 2023Article
- Opioid-Modulated Receptor Localization and Erk1/2 Phosphorylation in Cells Coexpressing μ-Opioid and Nociceptin Receptors.International journal of molecular sciences · 2023Article
- Structural basis for recognition of antihistamine drug by human histamine receptor.Nature communications · 2022Article
- Filling of a water-free void explains the allosteric regulation of the βNature chemistry · 2022Article
- Ptchd1 mediates opioid tolerance via cholesterol-dependent effects on μ-opioid receptor trafficking.Nature neuroscience · 2022Article
- Predictable cholesterol binding sites in GPCRs lack consensus motifs.Structure (London, England : 1993) · 2021Article
- A sensitive S-Trap-based approach to the analysis of T cell lipid raft proteome.Journal of lipid research · 2020Article
- Neuronal Signaling Involved in Neuronal Polarization and Growth: Lipid Rafts and Phosphorylation.Frontiers in molecular neuroscience · 2020Article
- Association between perioperative cholesterol level and analgesia after video-assisted thoracoscopic surgery.Korean journal of anesthesiology · 2019Observational
- GRK Mediates μ-Opioid Receptor Plasma Membrane Reorganization.Frontiers in molecular neuroscience · 2019Article
- Is preoperative hypocholesterolemia a risk factor for severe postoperative pain? Analysis of 1,944 patients after laparoscopic colorectal cancer surgery.Journal of pain research · 2018Article
- Prolonged Morphine Treatment Alters Expression and Plasma Membrane Distribution of β-Adrenergic Receptors and Some Other Components of Their Signaling System in Rat Cerebral Cortex.Journal of molecular neuroscience : MN · 2017Article
- Article
- Biased μ-opioid receptor agonists diversely regulate lateral mobility and functional coupling of the receptor to its cognate G proteins.Naunyn-Schmiedeberg's archives of pharmacology · 2016Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
μ-Opioid receptor (OPRM1) is mainly localized in lipid raft microdomains but internalizes through clathrin-dependent pathways. Our previous studies demonstrated that disruption of lipid rafts by cholesterol-depletion reagent blocked the agonist-induced internalization of OPRM1 and G protein-dependent signaling. The present study demonstrated that reduction of cholesterol level decreased and culturing cells in excess cholesterol increased the agonist-induced internalization and desensitization of OPRM1, respectively. Further analyses indicated that modulation of cellular cholesterol level did not affect agonist-induced receptor phosphorylation but did affect membrane translocation of β-arrestins. The translocation of β-arrestins was blocked by cholesterol reduction, and the effect could be reversed by incubating with cholesterol. OptiPrep gradient separation of lipid rafts revealed that excess cholesterol retained more receptors in lipid raft domains and facilitated the recruitment of β-arrestins to these microdomains upon agonist activation. Moreover, excess cholesterol could evoke receptor internalization and protein kinase C-independent extracellular signal-regulated kinases activation upon morphine treatment. Therefore, these results suggest that cholesterol not only can influence OPRM1 localization in lipid rafts but also can effectively enhance the recruitment of β-arrestins and thereby affect the agonist-induced trafficking and agonist-dependent signaling of OPRM1.
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