Crystallographic basis for calcium regulation of sodium channels

Proc Natl Acad Sci U S A. 2012 Feb 28;109(9):3558-63. doi: 10.1073/pnas.1114748109. Epub 2012 Feb 13.

Abstract

Voltage-gated sodium channels underlie the rapid regenerative upstroke of action potentials and are modulated by cytoplasmic calcium ions through a poorly understood mechanism. We describe the 1.35 Å crystal structure of Ca(2+)-bound calmodulin (Ca(2+)/CaM) in complex with the inactivation gate (DIII-IV linker) of the cardiac sodium channel (Na(V)1.5). The complex harbors the positions of five disease mutations involved with long Q-T type 3 and Brugada syndromes. In conjunction with isothermal titration calorimetry, we identify unique inactivation-gate mutations that enhance or diminish Ca(2+)/CaM binding, which, in turn, sensitize or abolish Ca(2+) regulation of full-length channels in electrophysiological experiments. Additional biochemical experiments support a model whereby a single Ca(2+)/CaM bridges the C-terminal IQ motif to the DIII-IV linker via individual N and C lobes, respectively. The data suggest that Ca(2+)/CaM destabilizes binding of the inactivation gate to its receptor, thus biasing inactivation toward more depolarized potentials.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Motifs
  • Amino Acid Sequence
  • Brugada Syndrome / genetics
  • Calcium / chemistry
  • Calcium / physiology*
  • Calmodulin / chemistry*
  • Calmodulin / physiology
  • Crystallography, X-Ray
  • Humans
  • Ion Channel Gating / physiology*
  • Long QT Syndrome / genetics
  • Macromolecular Substances
  • Membrane Potentials
  • Models, Molecular
  • Molecular Sequence Data
  • NAV1.5 Voltage-Gated Sodium Channel
  • Patch-Clamp Techniques
  • Protein Conformation
  • Protein Interaction Mapping
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry
  • Sequence Alignment
  • Sequence Homology, Amino Acid
  • Sodium / metabolism
  • Sodium Channels / chemistry*
  • Sodium Channels / physiology

Substances

  • CALM2 protein, human
  • Calmodulin
  • Macromolecular Substances
  • NAV1.5 Voltage-Gated Sodium Channel
  • Recombinant Fusion Proteins
  • SCN5A protein, human
  • Sodium Channels
  • Sodium
  • Calcium

Associated data

  • PDB/4DJC