ArticleScientific reports2016
Structural basis of TRPA1 inhibition by HC-030031 utilizing species-specific differences.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 66 citations in OpenAlex.
- Chemical Characterization and Pharmacological Activity of Byrsonima crassifolia (L.) Kunth (Murici): Antinociceptive Effects, Edema Reduction, and Molecular Docking.Chemistry & biodiversity · 2026Article
- Relationship between sensory irritation on skin surface and TRP channel activation.The journal of physiological sciences : JPS · 2026Article
- TRPA1 for Butterfly Eyespot Formation.International journal of molecular sciences · 2026Article
- Agonism of mosquito and human transient receptor potential ankyrin 1 (TRPA1) channels by the natural drimane sesquiterpene cinnamodial.bioRxiv : the preprint server for biology · 2025Article
- Stretch-Induced Increase in CaJournal of the American Heart Association · 2025Article
- Papillomavirus-like particles as vectors forMolecular therapy. Nucleic acids · 2025Article
- TRPA1 exacerbates selective retinal ganglion cell vulnerability under acute ocular hypertension.Acta neuropathologica communications · 2025Article
- Insights into Molecular Interactions and Biological Effect of Natural Stilbenoids at the TRPA1 Ion Channel.ChemMedChem · 2025Article
- Sea Anemone Kunitz Peptide HCIQ2c1: Structure, Modulation of TRPA1 Channel, and Suppression of Nociceptive Reaction In Vivo.Marine drugs · 2024Article
- Human Transient Receptor Potential Ankyrin 1 Channel: Structure, Function, and Physiology.Sub-cellular biochemistry · 2024Review
- Canine, mouse, and human transient receptor potential ankyrin 1 (TRPA1) channels show different sensitivity to menthol or cold stimulation.The Journal of veterinary medical science · 2023Article
- Discovery ofJournal of medicinal chemistry · 2023Article
- Stilbenoid compounds inhibit NF-κB-mediated inflammatory responses in theFrontiers in immunology · 2023Article
- The human TRPA1 intrinsic cold and heat sensitivity involves separate channel structures beyond the N-ARD domain.Nature communications · 2022Article
- Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity.Pharmacological reports : PR · 2022Article
- The Role of Saponins in the Treatment of Neuropathic Pain.Molecules (Basel, Switzerland) · 2022Review
- Structural Modeling of TRPA1 Ion Channel-Determination of the Binding Site for Antagonists.Molecules (Basel, Switzerland) · 2022Article
- Novel oxygen sensing mechanism in the spinal cord involved in cardiorespiratory responses to hypoxia.Science advances · 2022Article
- The Use of Zebrafish as a Non-traditional Model Organism in Translational Pain Research: The Knowns and the Unknowns.Current neuropharmacology · 2022Article
- Activation ofInternational journal of molecular sciences · 2021Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pain is a harmful sensation that arises from noxious stimuli. Transient receptor potential ankyrin 1 (TRPA1) is one target for studying pain mechanisms. TRPA1 is activated by various stimuli such as noxious cold, pungent natural products and environmental irritants. Since TRPA1 is an attractive target for pain therapy, a few TRPA1 antagonists have been developed and some function as analgesic agents. The responses of TRPA1 to agonists and antagonists vary among species and these species differences have been utilized to identify the structural basis of activation and inhibition mechanisms. The TRPA1 antagonist HC-030031 (HC) failed to inhibit frog TRPA1 (fTRPA1) and zebrafish TRPA1 activity induced by cinnamaldehyde (CA), but did inhibit human TRPA1 (hTRPA1) in a heterologous expression system. Chimeric studies between fTRPA1 and hTRPA1, as well as analyses using point mutants, revealed that a single amino acid residue (N855 in hTRPA1) significantly contributes to the inhibitory action of HC. Moreover, the N855 residue and the C-terminus region exhibited synergistic effects on the inhibition by HC. Molecular dynamics simulation suggested that HC stably binds to hTRPA1-N855. These findings provide novel insights into the structure-function relationship of TRPA1 and could lead to the development of more effective analgesics targeted to TRPA1.
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