ArticleACS chemical biology2013
An immunocytochemical-derived correlate for evaluating the bridging of heteromeric mu-delta opioid protomers by bivalent ligands.
Article in ACS chemical biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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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
18 citing papers in PubMed, 32 citations in OpenAlex.
- Opioid Analgesia and Opioid-Induced Adverse Effects: A Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- The size matters? A computational tool to design bivalent ligands.Bioinformatics (Oxford, England) · 2018Article
- Receptor-Receptor Interactions of G Protein-Coupled Receptors in the Carotid Body: A Working Hypothesis.Frontiers in physiology · 2018Article
- Basic/Translational Development of Forthcoming Opioid- and Nonopioid-Targeted Pain Therapeutics.Anesthesia and analgesia · 2017Review
- Breaking barriers to novel analgesic drug development.Nature reviews. Drug discovery · 2017Review
- A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NHACS chemical neuroscience · 2017Article
- Structure- and conformation-activity studies of nociceptin/orphanin FQ receptor dimeric ligands.Scientific reports · 2017Article
- Novel Molecular Strategies and Targets for Opioid Drug Discovery for the Treatment of Chronic Pain.The Yale journal of biology and medicine · 2017Review
- An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry · 2016Article
- Understanding the Functional Plasticity in Neural Networks of the Basal Ganglia in Cocaine Use Disorder: A Role for Allosteric Receptor-Receptor Interactions in A2A-D2 Heteroreceptor Complexes.Neural plasticity · 2016Review
- Ligand requirements for involvement of PKCε in synergistic analgesic interactions between spinal μ and δ opioid receptors.British journal of pharmacology · 2015Article
- Heteromers of μ-δ opioid receptors: new pharmacology and novel therapeutic possibilities.British journal of pharmacology · 2015Review
- Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochemical pharmacology · 2014Article
- Revolution in GPCR signalling: opioid receptor heteromers as novel therapeutic targets: IUPHAR review 10.British journal of pharmacology · 2014Review
- Antibodies to probe endogenous G protein-coupled receptor heteromer expression, regulation, and function.Frontiers in pharmacology · 2014Review
- Article
- Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB1) receptors are potent analgesics devoid of tolerance.Journal of medicinal chemistry · 2013Article
- Switching of delta opioid receptor subtypes in central amygdala microcircuits is associated with anxiety states in pain.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Bivalent ligands that contain two pharmacophores linked by a spacer are promising tools to investigate the pharmacology of opioid receptor heteromers. Evidence for occupation of neighboring protomers by two phamacophores of a single bivalent ligand (bridging) has relied mainly on pharmacological data. In the present study, we have employed an immunocytochemical correlate to support in vivo biological studies that are consistent with bridging. We show that a bivalent mu agonist/delta antagonist (MDAN-21) that is devoid of tolerance due to possible bridging of mu and delta protomers prevents endocytosis of the heteromeric receptors in HEK-293 cells. Conversely, a bivalent ligand (MDAN-16) with a short spacer or monovalent mu agonist give rise to robust internalization. The data suggest that the immobilization of proximal mu and delta protomers is due to bridging by MDAN-21. The finding that MDAN-21 and its shorter spacer homologue MDAN-16 possess equivalent activity in HEK-293 cells, but produce dramatically divergent internalization of mu-delta heteromer, is relevant to the role of internalization and tolerance.
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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.