A calcium sensor in the sodium channel modulates cardiac excitability

Nature. 2002 Jan 24;415(6870):442-7. doi: 10.1038/415442a.

Abstract

Sodium channels are principal molecular determinants responsible for myocardial conduction and maintenance of the cardiac rhythm. Calcium ions (Ca2+) have a fundamental role in the coupling of cardiac myocyte excitation and contraction, yet mechanisms whereby intracellular Ca2+ may directly modulate Na channel function have yet to be identified. Here we show that calmodulin (CaM), a ubiquitous Ca2+-sensing protein, binds to the carboxy-terminal 'IQ' domain of the human cardiac Na channel (hH1) in a Ca2+-dependent manner. This binding interaction significantly enhances slow inactivation-a channel-gating process linked to life-threatening idiopathic ventricular arrhythmias. Mutations targeted to the IQ domain disrupted CaM binding and eliminated Ca2+/CaM-dependent slow inactivation, whereas the gating effects of Ca2+/CaM were restored by intracellular application of a peptide modelled after the IQ domain. A naturally occurring mutation (A1924T) in the IQ domain altered hH1 function in a manner characteristic of the Brugada arrhythmia syndrome, but at the same time inhibited slow inactivation induced by Ca2+/CaM, yielding a clinically benign (arrhythmia free) phenotype.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Arrhythmias, Cardiac / metabolism
  • Binding Sites
  • Calcium / metabolism
  • Calmodulin / metabolism*
  • Electrophysiology
  • Humans
  • Ion Channel Gating
  • Molecular Sequence Data
  • Mutation
  • Myocardium / metabolism*
  • NAV1.5 Voltage-Gated Sodium Channel
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Sodium Channels / genetics
  • Sodium Channels / metabolism*
  • Syndrome
  • Ventricular Fibrillation / metabolism

Substances

  • Calmodulin
  • NAV1.5 Voltage-Gated Sodium Channel
  • Recombinant Fusion Proteins
  • SCN5A protein, human
  • Sodium Channels
  • Calcium