Structure and function of voltage-gated sodium channels at atomic resolution

Exp Physiol. 2014 Jan;99(1):35-51. doi: 10.1113/expphysiol.2013.071969. Epub 2013 Oct 4.

Abstract

Voltage-gated sodium channels initiate action potentials in nerve, muscle and other excitable cells. Early physiological studies described sodium selectivity, voltage-dependent activation and fast inactivation, and developed conceptual models for sodium channel function. This review article follows the topics of my 2013 Sharpey-Schafer Prize Lecture and gives an overview of research using a combination of biochemical, molecular biological, physiological and structural biological approaches that have elucidated the structure and function of sodium channels at the atomic level. Structural models for voltage-dependent activation, sodium selectivity and conductance, drug block and both fast and slow inactivation are discussed. A perspective for the future envisions new advances in understanding the structural basis for sodium channel function and the opportunity for structure-based discovery of novel therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Humans
  • Ion Channel Gating / drug effects
  • Ion Channel Gating / physiology
  • Protein Conformation
  • Sodium / metabolism
  • Sodium Channel Blockers / pharmacology
  • Voltage-Gated Sodium Channels / chemistry*
  • Voltage-Gated Sodium Channels / metabolism*

Substances

  • Sodium Channel Blockers
  • Voltage-Gated Sodium Channels
  • Sodium