ArticleEMBO reports2021
Structural mechanism of TRPV3 channel inhibition by the plant-derived coumarin osthole.
Article in EMBO reports, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers, 1 of them a synthesis that pooled it.
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Who cites it
37 citing papers in PubMed, 1 synthesis or guideline pooled it, 58 citations in OpenAlex.
- Signaling Pathways Involved in the Neuroprotective Effect of Osthole: Evidence and Mechanisms.Molecular neurobiology · 2024Pooled it
- Orally available Colivin traps TRPV3 in an inactive state and suppresses intestinal inflammation.The EMBO journal · 2026Article
- Design, synthesis and structural mechanism of action of TRPV1 agonist MSP20 with long-lasting analgesic effect.Nature communications · 2026Article
- Mechanisms of pruritus and advances in traditional Chinese medicine therapy (Review).Molecular medicine reports · 2026Review
- Structural diversity of heat-sensing channel TRPV3 with Olmsted syndrome mutations.Nature communications · 2026Article
- The locking mechanism of human TRPV6 inhibition by intracellular magnesium.Nature communications · 2025Article
- Advances in Atopic Dermatitis Treatment: From Pathogenesis to Natural Product-Based Therapies.Phytotherapy research : PTR · 2025Review
- Determinants for Activation of the Ion Channel TRPV3 by Weak Acids.International journal of molecular sciences · 2025Article
- Structural basis of the inhibition of TRPV1 by analgesic sesquiterpenes.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Molecular basis of TRPV3 channel blockade by intracellular polyamines.Communications biology · 2025Article
- Plant essential oil targets TRPV3 for skin renewal and structural mechanism of action.Nature communications · 2025Article
- The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids.International journal of molecular sciences · 2025Article
- Molecular and cellular mechanisms of itch sensation and the anti-itch drug targets.Acta pharmacologica Sinica · 2025Review
- Structure-function analyses of human TRPV6 ancestral and derived haplotypes.Structure (London, England : 1993) · 2025Article
- Article
- Conservation of the cooling agent binding pocket within the TRPM subfamily.bioRxiv : the preprint server for biology · 2024Article
- Inhibition of Cutaneous TRPV3 Channels by Natural Caffeic Acid for the Alleviation of Skin Inflammation.Molecules (Basel, Switzerland) · 2024Article
- TRPV3 activation by different agonists accompanied by lipid dissociation from the vanilloid site.Science advances · 2024Article
- Selective inhibition of overactive warmth-sensitive CaThe Journal of biological chemistry · 2024Article
- Pathogenesis and management ofFrontiers in genetics · 2024Review
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
TRPV3, a representative of the vanilloid subfamily of TRP channels, is predominantly expressed in skin keratinocytes and has been implicated in cutaneous sensation and associated with numerous skin pathologies and cancers. TRPV3 is inhibited by the natural coumarin derivative osthole, an active ingredient of Cnidium monnieri, which has been used in traditional Chinese medicine for the treatment of a variety of human diseases. However, the structural basis of channel inhibition by osthole has remained elusive. Here we present cryo-EM structures of TRPV3 in complex with osthole, revealing two types of osthole binding sites in the transmembrane region of TRPV3 that coincide with the binding sites of agonist 2-APB. Osthole binding converts the channel pore into a previously unidentified conformation with a widely open selectivity filter and closed intracellular gate. Our structures provide insight into competitive inhibition of TRPV3 by osthole and can serve as a template for the design of osthole chemistry-inspired drugs targeting TRPV3-associated diseases.
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