Powered by OpenAIRE graph
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/ Biophysical Journalarrow_drop_down
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/
Biophysical Journal
Article
License: Elsevier Non-Commercial
Data sources: UnpayWall
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/
Biophysical Journal
Article . 2007
License: Elsevier Non-Commercial
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/
image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao
Biophysical Journal
Article . 2007 . Peer-reviewed
License: Elsevier Non-Commercial
Data sources: Crossref
versions View all 4 versions

Sodium Channels: Ionic Model of Slow Inactivation and State-Dependent Drug Binding

Authors: Denis B. Tikhonov; Boris S. Zhorov;

Sodium Channels: Ionic Model of Slow Inactivation and State-Dependent Drug Binding

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.

Keywords

Ions, Cytoplasm, Sequence Homology, Amino Acid, Protein Conformation, Chemistry, Pharmaceutical, Molecular Sequence Data, Static Electricity, Biophysics, Molecular Conformation, Lidocaine, Sodium Channels, Electrochemistry, Animals, Amino Acid Sequence

  • BIP!
    Impact byBIP!
    citations
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    55
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
Powered by OpenAIRE graph
citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
55
Top 10%
Top 10%
Top 10%
hybrid