ArticleStructure (London, England : 1993)2011
Structural basis for μ-opioid receptor binding and activation.
Article in Structure (London, England : 1993), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 36 citations in OpenAlex.
- Population prevalence of high-risk pharmacogenetic configurations in a healthy older Australian reference cohort.Frontiers in pharmacology · 2026Article
- Serotonin release mediates analgesia via opioidergic system and withdrawal symptoms in chronic kratom extract-treated mice.BMC complementary medicine and therapies · 2025Article
- Development of 1,3-acetonedicarboxylate-derived glucoside amphiphiles (ACAs) for membrane protein study.Chemical science · 2022Article
- Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain.Journal of medicinal chemistry · 2021Article
- Conformationally flexible core-bearing detergents with a hydrophobic or hydrophilic pendant: Effect of pendant polarity on detergent conformation and membrane protein stability.Acta biomaterialia · 2021Article
- Identification and characterization of novel candidate compounds targeting 6- and 7-transmembrane μ-opioid receptor isoforms.British journal of pharmacology · 2021Article
- Haplotype-Based Association and In Silico Studies of OPRM1 Gene Variants with Susceptibility to Opioid Dependence Among Addicted Iranians Undergoing Methadone Treatment.Journal of molecular neuroscience : MN · 2020Article
- Molecular insights into the interaction of hemorphin and its targets.Scientific reports · 2019Article
- Stabilization of μ-opioid receptor facilitates its cellular translocation and signaling.Proteins · 2019Article
- μ Opioid receptor: novel antagonists and structural modeling.Scientific reports · 2016Article
- μ-Opioid receptor 6-transmembrane isoform: A potential therapeutic target for new effective opioids.Progress in neuro-psychopharmacology & biological psychiatry · 2015Review
- Cellular signalling of non-synonymous single-nucleotide polymorphisms of the human μ-opioid receptor (OPRM1).British journal of pharmacology · 2015Review
- Structural Determinants for the Binding of Morphinan Agonists to the μ-Opioid Receptor.PloS one · 2015Article
- Differential Regulation of 6- and 7-Transmembrane Helix Variants of μ-Opioid Receptor in Response to Morphine Stimulation.PloS one · 2015Article
- Pomegranate-derived anthocyanin regulates MORs-cAMP/CREB-BDNF pathways in opioid-dependent models and improves cognitive impairments.Journal of Ayurveda and integrative medicineArticle
- Mass Spectrometry Structural Proteomics Enabled by Limited Proteolysis and Cross-Linking.Mass spectrometry reviewsReview
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Opioids that stimulate the μ-opioid receptor (MOR1) are the most frequently prescribed and effective analgesics. Here we present a structural model of MOR1. Molecular dynamics simulations show a ligand-dependent increase in the conformational flexibility of the third intracellular loop that couples with the G protein complex. These simulations likewise identified residues that form frequent contacts with ligands. We validated the binding residues using site-directed mutagenesis coupled with radioligand binding and functional assays. The model was used to blindly screen a library of ∼1.2 million compounds. From the 34 compounds predicted to be strong binders, the top three candidates were examined using biochemical assays. One compound showed high efficacy and potency. Post hoc testing revealed this compound to be nalmefene, a potent clinically used antagonist, thus further validating the model. In summary, the MOR1 model provides a tool for elucidating the structural mechanism of ligand-initiated cell signaling and for screening novel analgesics.
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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.