ArticleChannels (Austin, Tex.)
State-independent intracellular access of quaternary ammonium blockers to the pore of TREK-1.
Article in Channels (Austin, Tex.). The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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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
28 citing papers in PubMed, 43 citations in OpenAlex.
- Effect of two activators on the gating of a KBiophysical journal · 2024Article
- Ion occupancy of the selectivity filter controls opening of a cytoplasmic gate in the KNature communications · 2024Article
- Structural Insights into the Mechanisms and Pharmacology of KJournal of molecular biology · 2021Review
- Norfluoxetine inhibits TREK-2 K2P channels by multiple mechanisms including state-independent effects on the selectivity filter gate.The Journal of general physiology · 2021Article
- TOK channels use the two gates in classical KFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Selectivity filter instability dominates the low intrinsic activity of the TWIK-1 K2P KThe Journal of biological chemistry · 2020Article
- Pharmacologically reversible, loss of function mutations in the TM2 and TM4 inner pore helices of TREK-1 K2P channels.Scientific reports · 2019Article
- Anchoring Property of a Novel Hydrophilic Lipopolymer, HDAS-SHP, Post-Inserted in Preformed Liposomes.Nanomaterials (Basel, Switzerland) · 2019Article
- A pharmacological master key mechanism that unlocks the selectivity filter gate in KScience (New York, N.Y.) · 2019Article
- Mechanism of Mechanosensitive Gating of the TREK-2 Potassium Channel.Biophysical journal · 2018Article
- Article
- Bilayer-Mediated Structural Transitions Control Mechanosensitivity of the TREK-2 K2P Channel.Structure (London, England : 1993) · 2017Article
- Markov modeling reveals novel intracellular modulation of the human TREK-2 selectivity filter.Scientific reports · 2017Article
- Pore size matters for potassium channel conductance.The Journal of general physiology · 2016Review
- Polymodal activation of the TREK-2 K2P channel produces structurally distinct open states.The Journal of general physiology · 2016Article
- Article
- Dominant-Negative Effect of a Missense Variant in the TASK-2 (KCNK5) K+ Channel Associated with Balkan Endemic Nephropathy.PloS one · 2016Article
- Calcium ions open a selectivity filter gate during activation of the MthK potassium channel.Nature communications · 2015Article
- Much more than a leak: structure and function of K₂p-channels.Pflugers Archiv : European journal of physiology · 2015Review
- Two-pore domain potassium channels: potential therapeutic targets for the treatment of pain.Pflugers Archiv : European journal of physiology · 2015Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 3 countries.
Funding
Abstract
We previously reported that TREK-1 gating by internal pH and pressure occurs close to or within the selectivity filter. These conclusions were based upon kinetic measurements of high-affinity block by quaternary ammonium (QA) ions that appeared to exhibit state-independent accessibility to their binding site within the pore. Intriguingly, recent crystal structures of two related K2P potassium channels were also both found to be open at the helix bundle crossing. However, this did not exclude the possibility of gating at the bundle crossing and it was suggested that side-fenestrations within these structures might allow state-independent access of QA ions to their binding site. In this addendum to our original study we demonstrate that even hydrophobic QA ions do not access the TREK-1 pore via these fenestrations. Furthermore, by using a chemically reactive QA ion immobilized within the pore via covalent cysteine modification we provide additional evidence that the QA binding site remains accessible to the cytoplasm in the closed state. These results support models of K2P channel gating which occur close to or within the selectivity filter and do not involve closure at the helix bundle crossing.
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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.