ArticleScience advances2024
TRPV3 activation by different agonists accompanied by lipid dissociation from the vanilloid site.
Article in Science advances, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 38 citations in OpenAlex.
- Avicularin and Senegenin Suppress TRPV3-Associated TSLP Expression in Human Keratinocytes.Cells · 2026Article
- Orally available Colivin traps TRPV3 in an inactive state and suppresses intestinal inflammation.The EMBO journal · 2026Article
- Structural origins of species-specific differences in TRPV2 activation.Nature communications · 2026Article
- Design, synthesis and structural mechanism of action of TRPV1 agonist MSP20 with long-lasting analgesic effect.Nature communications · 2026Article
- Expression and functional characterization of the TRPV3 channel in domestic cat (Felis catus) mature oocytes.Biological research · 2026Article
- Structural diversity of heat-sensing channel TRPV3 with Olmsted syndrome mutations.Nature communications · 2026Article
- Thermodynamic coupling between cold and heat activations of TRPV2.Scientific reports · 2026Article
- Open-channel block of human TRPV6 by polyamine spermine.Nature communications · 2026Article
- Temperature-dependent gating pathways in TRPV3.Scientific reports · 2026Article
- Visualizing insecticide control of insect TRP channel function and assembly.Nature communications · 2025Article
- Examining the thermotropic properties of large circularized nanodiscs.Biochimica et biophysica acta. Biomembranes · 2025Article
- Pathway-dependent cold activation of heat-responsive TRPV channels.Scientific reports · 2025Article
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- Article
- 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
- Structural insights into TRPV2 modulation by probenecid.Nature structural & molecular biology · 2025Article
- Structural dynamics and permeability of the TRPV3 pentamer.Nature communications · 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
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
TRPV3 represents both temperature- and ligand-activated transient receptor potential (TRP) channel. Physiologically relevant opening of TRPV3 channels by heat has been captured structurally, while opening by agonists has only been observed in structures of mutant channels. Here, we present cryo-EM structures that illuminate opening and inactivation of wild-type human TRPV3 in response to binding of two types of agonists: either the natural cannabinoid tetrahydrocannabivarin (THCV) or synthetic agonist 2-aminoethoxydiphenylborane (2-APB). We found that THCV binds to the vanilloid site, while 2-APB binds to the S1-S4 base and ARD-TMD linker sites. Despite binding to distally located sites, both agonists induce similar pore opening and cause dissociation of a lipid that occupies the vanilloid site in their absence. Our results uncover different but converging allosteric pathways through which small-molecule agonists activate TRPV3 and provide a framework for drug design and understanding the role of lipids in ion channel function.
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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.