ArticleThe Journal of biological chemistry2010
Farnesyl pyrophosphate is a novel pain-producing molecule via specific activation of TRPV3.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 68 papers.
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Who cites it
68 citing papers in PubMed, 131 citations in OpenAlex.
- Orally available Colivin traps TRPV3 in an inactive state and suppresses intestinal inflammation.The EMBO journal · 2026Article
- Article
- Role of transient receptor potential channels on pathogenesis and treatment of psoriasis.Inflammopharmacology · 2026Review
- Characterization of the Functional Transient Receptor Potential Vanilloid Channels 1 to 4 in Human Corneal Endothelial Cells.Investigative ophthalmology & visual science · 2026Article
- A pathway to next-generation mast cell stabilizers identified through the novel Phytomedical Analytics for Research Optimization at scale data platform.Frontiers in pharmacology · 2026Article
- A pathway to next-generation mast cell stabilizers identified through the novel Phytomedical Analytics for Research Optimization at Scale data platform.bioRxiv : the preprint server for biology · 2025Article
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- TNF inhibitors target a mevalonate metabolite/TRPM2/calcium signaling axis in neutrophils to dampen vasculitis in Behçet's disease.Nature communications · 2024Article
- Preliminary investigation on the establishment of a new meibomian gland obstruction model and gene expression.Scientific reports · 2024Article
- Pathogenesis and management ofFrontiers in genetics · 2024Review
- Role of TRP Channels in Liver-Related Diseases.International journal of molecular sciences · 2023Review
- TRPV3 Ion Channel: From Gene to Pharmacology.International journal of molecular sciences · 2023Review
- Novel Insights into the Role of Keratinocytes-Expressed TRPV3 in the Skin.Biomolecules · 2023Review
- TRPV3: Structure, Diseases and Modulators.Molecules (Basel, Switzerland) · 2023Review
- Regulation of ThermoTRP Channels by PIP2 and Cholesterol.Advances in experimental medicine and biology · 2023Article
- Structural mechanism of TRPV3 channel inhibition by the anesthetic dyclonine.Nature communications · 2022Article
- Inhibition of temperature-sensitive TRPV3 channel by two natural isochlorogenic acid isomers for alleviation of dermatitis and chronic pruritus.Acta pharmaceutica Sinica. B · 2022Article
- Emerging roles of keratinocytes in nociceptive transduction and regulation.Frontiers in molecular neuroscience · 2022Review
- Farnesyl pyrophosphate is a new danger signal inducing acute cell death.PLoS biology · 2021Article
- TRPing to the Point of Clarity: Understanding the Function of the Complex TRPV4 Ion Channel.Cells · 2021Review
8 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Temperature-sensitive transient receptor potential ion channels (thermoTRPs) expressed in epidermal keratinocytes and sensory afferents play an important role as peripheral pain detectors for our body. Many natural and synthetic compounds have been found to act on the thermoTRPs leading to altered nociception, but little is known about endogenous painful molecules activating TRPV3. Here, we show that farnesyl pyrophosphate (FPP), an intermediate metabolite in the mevalonate pathway, specifically activates TRPV3 among six thermoTRPs using Ca(2+) imaging and electrophysiology with cultured keratinocytes and TRPV3-overexpressing cells. Agonistic potencies of related compounds in the FPP metabolism were ignorable. Voltage-dependence of TRPV3 was shifted by FPP, which appears to be the activation mechanism. An intraplantar injection of FPP acutely elicits nociceptive behaviors in inflamed animals, indicating that FPP is a novel endogenous pain-producing substance via TRPV3 activation. Co-culture experiments demonstrated that this FPP-evoked signal in the keratinocytes is transmitted to sensory neurons. In addition, FPP reduced TRPV3 heat threshold resulting in heightened behavioral sensitivity to noxious heat. Taken together, our data suggest that FPP is the firstly identified endogenous TRPV3 activator that causes nociception. Our results may provide useful chemical information to elucidate TRPV3 physiology and novel pain-related metabolisms.
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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.