ArticleBiophysical journal2007
Sodium channels: ionic model of slow inactivation and state-dependent drug binding.
Article in Biophysical journal, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed.
- Allergy to Local Anesthetics is a Rarity: Review of Diagnostics and Strategies for Clinical Management.Clinical reviews in allergy & immunology · 2023Review
- Modulation of Slow Desensitization (Tachyphylaxis) of Acid-Sensing Ion Channel (ASIC)1a.Cellular and molecular neurobiology · 2023Article
- Possible Interactions of Extracellular Loop IVP2-S6 With Voltage-Sensing Domain III in Cardiac Sodium Channel.Frontiers in pharmacology · 2021Article
- Elucidation of pyrethroid and DDT receptor sites in the voltage-gated sodium channel.Neurotoxicology · 2017Review
- Mechanism of sodium channel block by local anesthetics, antiarrhythmics, and anticonvulsants.The Journal of general physiology · 2017Article
- Molecular Mechanism of Action and Selectivity of Sodium Ch annel Blocker Insecticides.Current medicinal chemistry · 2017Review
- The Receptor Site and Mechanism of Action of Sodium Channel Blocker Insecticides.The Journal of biological chemistry · 2016Article
- Mutations in the transmembrane helix S6 of domain IV confer cockroach sodium channel resistance to sodium channel blocker insecticides and local anesthetics.Insect biochemistry and molecular biology · 2015Article
- State-dependent inter-repeat contacts of exceptionally conserved asparagines in the inner helices of sodium and calcium channels.Pflugers Archiv : European journal of physiology · 2015Article
- A mutation in the intracellular loop III/IV of mosquito sodium channel synergizes the effect of mutations in helix IIS6 on pyrethroid resistance.Molecular pharmacology · 2015Article
- Folding similarity of the outer pore region in prokaryotic and eukaryotic sodium channels revealed by docking of conotoxins GIIIA, PIIIA, and KIIIA in a NavAb-based model of Nav1.4.The Journal of general physiology · 2014Article
- Molecular biology of insect sodium channels and pyrethroid resistance.Insect biochemistry and molecular biology · 2014Article
- Voltage-Gated Sodium Channels as Insecticide Targets.Advances in insect physiology · 2014Article
- A naturally occurring amino acid substitution in the voltage-dependent sodium channel selectivity filter affects channel gating.Journal of comparative physiology. A, Neuroethology, sensory, neural, and behavioral physiology · 2013Article
- Indoxacarb, Metaflumizone, and Other Sodium Channel Inhibitor Insecticides: Mechanism and Site of Action on Mammalian Voltage-Gated Sodium Channels.Pesticide biochemistry and physiology · 2013Article
- Energy for wild-type acetylcholine receptor channel gating from different choline derivatives.Biophysical journal · 2013Article
- Ionic channels as targets for drug design: a review on computational methods.Pharmaceutics · 2011Article
- Identification of new batrachotoxin-sensing residues in segment IIIS6 of the sodium channel.The Journal of biological chemistry · 2011Article
- Possible roles of exceptionally conserved residues around the selectivity filters of sodium and calcium channels.The Journal of biological chemistry · 2011Article
- Overlapping binding sites of structurally different antiarrhythmics flecainide and propafenone in the subunit interface of potassium channel Kv2.1.The Journal of biological chemistry · 2010Article
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2 authors.
Funding
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Abstract
Inactivation is a fundamental property of voltage-gated ion channels. Fast inactivation of Na(+) channels involves channel block by the III-IV cytoplasmic interdomain linker. The mechanisms of nonfast types of inactivation (intermediate, slow, and ultraslow) are unclear, although the ionic environment and P-loops rearrangement appear to be involved. In this study, we employed a TTX-based P-loop domain model of a sodium channel and the MCM method to investigate a possible role of P-loop rearrangement in the nonfast inactivation. Our modeling predicts that Na(+) ions can bind between neighboring domains in the outer-carboxylates ring EEDD, forming an ordered structure with interdomain contacts that stabilize the conducting conformation of the outer pore. In this model, the permeant ions can transit between the EEDD ring and the selectivity filter ring DEKA, retaining contacts with at least two carboxylates. In the absence of Na(+), the electrostatic repulsion between the EEDD carboxylates disrupts the permeable configuration. In this Na(+)-deficient model, the region between the EEDD and DEKA rings is inaccessible for Na(+) but is accessible for TMA. Taken together, these results suggest that Na(+)-saturated models are consistent with experimental characteristics of the open channels, whereas Na(+)-deficient models are consistent with experimentally defined properties of the slow-inactivated channels. Our calculations further predict that binding of LAs to the inner pore would depend on whether Na(+) occupies the DEKA ring. In the absence of Na(+) in the DEKA ring, the cationic group of lidocaine occurs in the focus of the pore helices' macrodipoles and would prevent occupation of the ring by Na(+). Loading the DEKA ring with Na(+) results in the electrostatic repulsion with lidocaine. Thus, there are antagonistic relations between a cationic ligand bound in the inner pore and Na(+) in the DEKA ring.
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