ArticleFASEB journal : official publication of the Federation of American Societies for Experimental Biology2019
Stereochemistry and innate immune recognition: (+)-norbinaltorphimine targets myeloid differentiation protein 2 and inhibits toll-like receptor 4 signaling.
Article in FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 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
6 citing papers in PubMed, 21 citations in OpenAlex.
- Myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS): diagnosis and management.Journal of translational medicine · 2025Review
- Recent Advances in Studying Toll-like Receptors with the Use of Computational Methods.Journal of chemical information and modeling · 2023Review
- Toll-like Receptors and Thrombopoiesis.International journal of molecular sciences · 2023Review
- Nicotine and its metabolite cotinine target MD2 and inhibit TLR4 signaling.Innovation (Cambridge (Mass.)) · 2021Article
- Potential Roles of Myeloid Differentiation Factor 2 on Neuroinflammation and Its Possible Interventions.Molecular neurobiology · 2020Review
- Toll-Like Receptor 4 (TLR4)/Opioid Receptor Pathway Crosstalk and Impact on Opioid Analgesia, Immune Function, and Gastrointestinal Motility.Frontiers in immunology · 2020Review
Corrections and comments
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Authors and funding
14 authors at 10 institutions in 3 countries.
Funding
Abstract
Deregulation of innate immune TLR4 signaling contributes to various diseases including neuropathic pain and drug addiction. Naltrexone is one of the rare TLR4 antagonists with good blood-brain barrier permeability and showing no stereoselectivity for TLR4. By linking 2 naltrexone units through a rigid pyrrole spacer, the bivalent ligand norbinaltorphimine was formed. Interestingly, (+)-norbinaltorphimine [(+)-1] showed ∼25 times better TLR4 antagonist activity than naltrexone in microglial BV-2 cell line, whereas (-)-norbinaltorphimine [(-)-1] lost TLR4 activity. The enantioselectivity of norbinaltorphimine was further confirmed in primary microglia, astrocytes, and macrophages. The activities of meso isomer of norbinaltorphimine and the molecular dynamic simulation results demonstrate that the stereochemistry of (+)-1 is derived from the (+)-naltrexone pharmacophore. Moreover, (+)-1 significantly increased and prolonged morphine analgesia
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Registered trials
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