ArticleScientific reports2016
Selective potentiation of 2-APB-induced activation of TRPV1-3 channels by acid.
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 26 papers.
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Who cites it
26 citing papers in PubMed, 37 citations in OpenAlex.
- Nongenomic Stimulatory Effect of T3 on Calcium Dynamics in GnRH Neurons via Integrin αVβ3.Endocrinology · 2025Article
- Determinants for Activation of the Ion Channel TRPV3 by Weak Acids.International journal of molecular sciences · 2025Article
- Article
- The TRPV3 channel is a mediator of zinc influx and homeostasis in murine oocytes.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Prebiotics as modulators of colonic calcium and magnesium uptake.Acta physiologica (Oxford, England) · 2025Review
- TRPV2 calcium channel promotes breast cancer progression potential by activating autophagy.Cancer cell international · 2024Article
- Functional and structural insights into activation of TRPV2 by weak acids.The EMBO journal · 2024Article
- Article
- The calcium channel modulator 2-APB hydrolyzes in physiological buffers and acts as an effective radical scavenger and inhibitor of the NADPH oxidase 2.Redox biology · 2023Article
- Cannabidiol sensitizes TRPV2 channels to activation by 2-APB.bioRxiv : the preprint server for biology · 2023Article
- Targeting TRP channels: recent advances in structure, ligand binding, and molecular mechanisms.Frontiers in molecular neuroscience · 2023Review
- CaInternational journal of molecular sciences · 2022Review
- Inhibition of intracellular proton-sensitive CaActa pharmaceutica Sinica. B · 2022Article
- Effects of butyratePflugers Archiv : European journal of physiology · 2022Article
- Gonococcal invasion into epithelial cells depends on both cell polarity and ezrin.PLoS pathogens · 2021Article
- Article
- Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine.eLife · 2021Article
- Mechanisms of proton inhibition and sensitization of the cation channel TRPV3.The Journal of general physiology · 2021Article
- Article
- Intracellular acidification facilitates receptor-operated TRPC4 activation through PLCδ1 in a CaThe Journal of physiology · 2020Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
Abstract
Temperature-sensitive TRP channels are important for responses to pain and inflammation, to both of which tissue acidosis is a major contributing factor. However, except for TRPV1, acid-sensing by other ThermoTRP channels remains mysterious. We show here that unique among TRPV1-3 channels, TRPV3 is directly activated by protons from cytoplasmic side. This effect is very weak and involves key cytoplasmic residues L508, D512, S518, or A520. However, mutations of these residues did not affect a strong proton induced potentiation of TRPV3 currents elicited by the TRPV1-3 common agonist, 2-aminoethoxydiphenyl borate (2-APB), no matter if the ligand was applied from extracellular or cytoplasmic side. The acid potentiation was common among TRPV1-3 and only seen with 2-APB-related ligands. Using (1)H-nuclear magnetic resonance to examine the solution structures of 2-APB and its analogs, we observed striking structural differences of the boron-containing compounds at neutral/basic as compared to acidic pH, suggesting that a pH-dependent configuration switch of 2-APB-based drugs may underlie their functionality. Supporting this notion, protons also enhanced the inhibitory action of 2-APB on TRPM8. Collectively, our findings reveal novel insights into 2-APB action on TRP channels, which should facilitate the design of new drugs for these channels.
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Registered trials
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