ArticleScientific reports2018
Molecular details of dimerization kinetics reveal negligible populations of transient µ-opioid receptor homodimers at physiological concentrations.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 50 citations in OpenAlex.
- Single-molecule methods for characterizing receptor dimers reveal metastable opioid receptor homodimers that induce functional modulation.Nature communications · 2025Article
- Single-molecule characterization of opioid receptor heterodimers reveals soluble µ-δ dimer blocker peptide alleviates morphine tolerance.Nature communications · 2025Article
- Article
- The Role of Cholesterol in M2 Clustering and Viral Budding Explained.Journal of chemical theory and computation · 2025Article
- Computational drug development for membrane protein targets.Nature biotechnology · 2024Review
- Structural basis of dimerization of chemokine receptors CCR5 and CXCR4.Nature communications · 2023Article
- Dimerization of melanocortin 4 receptor controls puberty onset and body size polymorphism.Frontiers in endocrinology · 2023Article
- Computationally designed GPCR quaternary structures bias signaling pathway activation.Nature communications · 2022Article
- Preferential Gs protein coupling of the galanin GalPharmacological research · 2022Article
- The MProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Estimation of binding rates and affinities from multiensemble Markov models and ligand decoupling.The Journal of chemical physics · 2022Article
- Modulation of adenosine A2a receptor oligomerization by receptor activation and PIPStructure (London, England : 1993) · 2021Article
- Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.Journal of medicinal chemistry · 2021Article
- Article
- Single-molecule FRET imaging of GPCR dimers in living cells.Nature methods · 2021Article
- A critical perspective on Markov state model treatments of protein-protein association using coarse-grained simulations.The Journal of chemical physics · 2021Article
- Allosteric Modulation of GPCRs of Class A by Cholesterol.International journal of molecular sciences · 2021Review
- Interclass GPCR heteromerization affects localization and trafficking.Science signaling · 2020Article
- Exploring the activation pathway and GProceedings of the National Academy of Sciences of the United States of America · 2020Article
- Single-molecule analysis reveals agonist-specific dimer formation of µ-opioid receptors.Nature chemical biology · 2020Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
Various experimental and computational techniques have been employed over the past decade to provide structural and thermodynamic insights into G Protein-Coupled Receptor (GPCR) dimerization. Here, we use multiple microsecond-long, coarse-grained, biased and unbiased molecular dynamics simulations (a total of ~4 milliseconds) combined with multi-ensemble Markov state models to elucidate the kinetics of homodimerization of a prototypic GPCR, the µ-opioid receptor (MOR), embedded in a 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC)/cholesterol lipid bilayer. Analysis of these computations identifies kinetically distinct macrostates comprising several different short-lived dimeric configurations of either inactive or activated MOR. Calculated kinetic rates and fractions of dimers at different MOR concentrations suggest a negligible population of MOR homodimers at physiological concentrations, which is supported by acceptor photobleaching fluorescence resonance energy transfer (FRET) experiments. This study provides a rigorous, quantitative explanation for some conflicting experimental data on GPCR oligomerization.
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