ArticleEuropean journal of pharmacology2013
Ligand interaction, binding site and G protein activation of the mu opioid receptor.
Article in European journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 35 citations in OpenAlex.
- Indole Alkaloids as Biased Opioid Receptor Modulators.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Total synthesis and biological activity of "carbamorphine": O-to-CHProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs.International journal of molecular sciences · 2021Review
- Novel variants of engineered water soluble mu opioid receptors with extensive mutations and removal of cysteines.Proteins · 2021Article
- Predicting the Membrane Permeability of Fentanyl and Its Analogues by Molecular Dynamics Simulations.The journal of physical chemistry. B · 2021Article
- Ketamine Metabolite (2ACS chemical neuroscience · 2021Article
- Identification and characterization of plant-derived alkaloids, corydine and corydaline, as novel mu opioid receptor agonists.Scientific reports · 2020Article
- Mechanistic Understanding of Peptide Analogues, DALDA, [DmtMolecules (Basel, Switzerland) · 2020Article
- The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics.Frontiers in chemistry · 2020Review
- Molecular insights into the interaction of hemorphin and its targets.Scientific reports · 2019Article
- Water Soluble G-protein Coupled Receptor Enabled Biosensors.Translational perioperative and pain medicine · 2019Article
- Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?Drug discovery today · 2017Review
- Convergent Balancing Selection on the Mu-Opioid Receptor in Primates.Molecular biology and evolution · 2017Article
- Molecular Docking, Molecular Dynamics, and Structure-Activity Relationship Explorations of 14-Oxygenated N-Methylmorphinan-6-ones as Potent μ-Opioid Receptor Agonists.ACS chemical neuroscience · 2017Article
- Drug Binding Poses Relate Structure with Efficacy in the μ Opioid Receptor.Journal of molecular biology · 2017Article
- Characterization of a computationally designed water-soluble human μ-opioid receptor variant using available structural information.Anesthesiology · 2014Article
- On the modularity of the intrinsic flexibility of the µ opioid receptor: a computational study.PloS one · 2014Article
Corrections and comments
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Authors and funding
3 authors at 3 institutions in 2 countries.
Funding
Abstract
With the recently solved crystal structure of the murine mu opioid receptor, the elucidation of the structure function relationships of the human mu receptor becomes feasible. In this study, we analyzed the available structural information along with ligand binding and G protein activation of human mu receptor. Affinity determinations were performed in a HEK293 cell line stably transfected with the human mu opioid receptor for 6 different agonists (morphine, DMAGO, and herkinorn) and antagonists (naloxone, beta-Funaltrexamine, and Norbinaltorphimine). G protein activation was investigated in membrane preparations containing human mu receptors treated with the agonist, partial agonist, or antagonist compounds. 4DKL.pdb was utilized for structural analysis and docking calculations for 28 mu receptor ligands. The predicted affinities from docking were compared with those experimentally determined. While all known ligands bind to the receptor through the same binding site that is large enough to accommodate molecules of various sizes, interaction with D147 (D149 in human mu receptor) is essential for binding. No distinguishable interaction pattern in the binding site for agonist, partial agonist, or antagonist to predict pharmacological activities was found. The failure to reconcile the predicted affinities from docking with experimental values indicates that the receptor might undergo significant conformational changes from one state to the other states upon different ligand binding. A simplified model to understand the complicated system is proposed and further study on these multiple conformations using high resolution structural approaches is suggested.
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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.