ArticleThe Journal of general physiology2014
Divalent cations activate TRPV1 through promoting conformational change of the extracellular region.
Article in The Journal of general physiology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
33 citing papers in PubMed, 1 synthesis or guideline pooled it, 54 citations in OpenAlex.
- Centipede Venom Peptides Acting on Ion Channels.Toxins · 2020Pooled it
- Review
- Insights into ion channels to identify drug target for neuropathic pain management.Inflammopharmacology · 2025Review
- Dual Role of TRPV1 Channels in Cerebral Stroke: An Exploration from a Mechanistic and Therapeutic Perspective.Molecular neurobiology · 2024Review
- Temperature-Dependent Activation of Thermosensitive Transient Receptor Potential Channels.Advances in experimental medicine and biology · 2024Review
- Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand-Target Interaction.Plants (Basel, Switzerland) · 2023Review
- Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia.Nature communications · 2023Article
- A bibliometrics analysis and visualization study of TRPV1 channel.Frontiers in pharmacology · 2023Review
- Article
- Lipid-dependent sequential allosteric activation of heat-sensing TRPV1 channels by anchor-stereoselective "hot" vanilloid compounds and analogs.Biochemistry and biophysics reports · 2021Review
- Rational Design of a Modality-Specific Inhibitor of TRPM8 Channel against Oxaliplatin-Induced Cold Allodynia.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2021Article
- TRPV1: Role in Skin and Skin Diseases and Potential Target for Improving Wound Healing.International journal of molecular sciences · 2021Review
- An Unorthodox Mechanism Underlying Voltage Sensitivity of TRPV1 Ion Channel.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Article
- A specialized pore turret in the mammalian cation channel TRPV1 is responsible for distinct and species-specific heat activation thresholds.The Journal of biological chemistry · 2020Article
- TRPV1: Structure, Endogenous Agonists, and Mechanisms.International journal of molecular sciences · 2020Review
- A centipede toxin causes rapid desensitization of nociceptor TRPV1 ion channel.Toxicon : official journal of the International Society on Toxinology · 2020Article
- TRP ion channels: Proteins with conformational flexibility.Channels (Austin, Tex.) · 2019Review
- Cnnm4 deficiency suppresses CaOncogene · 2019Article
- Structures of TRPV2 in distinct conformations provide insight into role of the pore turret.Nature structural & molecular biology · 2019Article
- Inflammation, Cancer and Immunity-Implication of TRPV1 Channel.Frontiers in oncology · 2019Review
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 3 countries.
Funding
Abstract
Divalent cations Mg(2+) and Ba(2+) selectively and directly potentiate transient receptor potential vanilloid type 1 heat activation by lowering the activation threshold into the room temperature range. We found that Mg(2+) potentiates channel activation only from the extracellular side; on the intracellular side, Mg(2+) inhibits channel current. By dividing the extracellularly accessible region of the channel protein into small segments and perturbing the structure of each segment with sequence replacement mutations, we observed that the S1-S2 linker, the S3-S4 linker, and the pore turret are all required for Mg(2+) potentiation. Sequence replacements at these regions substantially reduced or eliminated Mg(2+)-induced activation at room temperature while sparing capsaicin activation. Heat activation was affected by many, but not all, of these structural alternations. These observations indicate that extracellular linkers and the turret may interact with each other. Site-directed fluorescence resonance energy transfer measurements further revealed that, like heat, Mg(2+) also induces structural changes in the pore turret. Interestingly, turret movement induced by Mg(2+) precedes channel activation, suggesting that Mg(2+)-induced conformational change in the extracellular region most likely serves as the cause of channel activation instead of a coincidental or accommodating structural adjustment.
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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.