ArticleBritish journal of pharmacology2001
Pharmacological modulation of monovalent cation currents through the epithelial Ca2+ channel ECaC1.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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44 citing papers in PubMed, 119 citations in OpenAlex.
- [Advances in the development of transient receptor potential melastatin 2 channel inhibitors].Zhejiang da xue xue bao. Yi xue ban = Journal of Zhejiang University. Medical sciences · 2025Review
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- A novel TRPV5/6-like channel from a scleractinian coral.PloS one · 2025Article
- Structural mechanism of TRPV5 inhibition by econazole.Structure (London, England : 1993) · 2024Article
- Molecular details of ruthenium red pore block in TRPV channels.EMBO reports · 2024Article
- Molecular pharmacology of the onco-TRP channel TRPV6.Channels (Austin, Tex.) · 2023Review
- Structural mechanism of human oncochannel TRPV6 inhibition by the natural phytoestrogen genistein.Nature communications · 2023Article
- Targeting ion channels with ultra-large library screening for hit discovery.Frontiers in molecular neuroscience · 2023Review
- Cell death induction and protection by activation of ubiquitously expressed anion/cation channels. Part 3: the roles and properties of TRPM2 and TRPM7.Frontiers in cell and developmental biology · 2023Review
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- Ligand-Binding Sites in Vanilloid-Subtype TRP Channels.Frontiers in pharmacology · 2022Review
- Applications of Cryo-EM in small molecule and biologics drug design.Biochemical Society transactions · 2021Article
- Structural mechanisms of TRPV6 inhibition by ruthenium red and econazole.Nature communications · 2021Article
- TRPV6 as A Target for Cancer Therapy.Journal of Cancer · 2020Review
- TRP ion channels: Proteins with conformational flexibility.Channels (Austin, Tex.) · 2019Review
- Article
- Structural basis of TRPV5 channel inhibition by econazole revealed by cryo-EM.Nature structural & molecular biology · 2018Article
- A Gate Hinge Controls the Epithelial Calcium Channel TRPV5.Scientific reports · 2017Article
- Divalent heavy metal cations block the TRPV1 Ca(2+) channel.Biological trace element research · 2013Article
- The action of selective CRAC channel blockers is affected by the Orai pore geometry.Cell calcium · 2013Article
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The recent identification of the epithelial Ca(2+) channel, ECaC1, represents a major step forward in our knowledge of renal Ca(2+) handling. ECaC1 constitutes the rate-limiting apical Ca(2+) entry mechanism of active, transcellular Ca(2+) reabsorption. This unique highly selective Ca(2+) channel shares a low but significant homology with transient receptor potential (TRP) channels and vanilloid receptors (VR). 2. We have studied the pharmacological modulation of currents through ECaC1 heterologously expressed in HEK 293 cells. Monovalent cation currents were measured by use of the whole cell patch clamp technique in cells dialysed with 10 mM BAPTA or 10 mM EGTA to prevent the fast Ca(2+) dependent inactivation of ECaC1. 3. Several modulators were tested, including inorganic cations, putative store-operated Ca(2+) entry (SOC) blockers, the vanilloid receptor (VR-1) blocker capsazepine, protein tyrosine kinase blockers, calmodulin antagonists and ruthenium red. 4. Ruthenium red and econazole appeared to be the most effective inhibitors of currents through ECaC1, with IC(50) values of 111 nM and 1.3 microM, respectively, whereas the selective SOC inhibitor, SKF96365, was nearly ineffective. 5. The divalent cation current block profile for ECaC1 is Pb(2+)=Cu(2+) >Zn(2+) >Co(2+) >Fe(2+) with IC(50) values between 1 and approximately 10 microM. 6. In conclusion, ECaC activity is effectively inhibited by various compounds including ruthenium red, antimycotic drugs and divalent cations, which might be useful tools for pharmacological manipulation and several disorders related to Ca(2+) homeostasis could benefit from such developments.
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