Constitutively active adenosine monophosphate-activated protein kinase regulates voltage-gated sodium channels in ventricular myocytes

Circulation. 2003 Apr 22;107(15):1962-5. doi: 10.1161/01.CIR.0000069269.60167.02. Epub 2003 Apr 7.

Abstract

Background: Some PRKAG2 mutations in the human gene encoding for the gamma-subunit of the adenosine monophosphate-activated protein kinase (AMPK) recently have been shown to cause rhythm disturbances (often fatal) in affected patients.

Methods and results: Rat ventricular myocytes were infected with an adenoviral vector designed to express a truncated constitutively active mutant (T172D) of the AMPK alpha1-subunit (CA-AMPK). The human cardiac sodium channel hH1 and CA-AMPK were also coexpressed in a mammalian cell line. Patch-clamp techniques were used to measure myocyte action potentials and recombinant hH1 sodium channel currents. Our results demonstrate that action potential duration is significantly prolonged in myocytes expressing the CA-AMPK construct, leading to the production of potentially arrhythmogenic early afterdepolarizations. Recombinant sodium channel current analysis revealed that expression of CA-AMPK significantly slowed open-state inactivation and shifted the voltage-activation curve in a hyperpolarizing direction.

Conclusions: We propose that sodium channels may be substrates for AMPK, possibly contributing to the observed arrhythmogenic activity in patients with some PRKAG2 mutations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AMP-Activated Protein Kinases
  • Action Potentials / physiology
  • Amino Acid Substitution
  • Animals
  • Arrhythmias, Cardiac / genetics
  • Cells, Cultured
  • Enzyme Activation / genetics
  • Heart Ventricles / cytology*
  • Humans
  • Multienzyme Complexes / genetics
  • Multienzyme Complexes / metabolism*
  • Myocytes, Cardiac / cytology
  • Myocytes, Cardiac / metabolism*
  • Patch-Clamp Techniques
  • Protein Serine-Threonine Kinases / genetics
  • Protein Serine-Threonine Kinases / metabolism*
  • Protein Subunits / genetics
  • Protein Subunits / metabolism
  • Rats
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Sodium Channels / genetics
  • Sodium Channels / metabolism*
  • Transfection

Substances

  • Multienzyme Complexes
  • Protein Subunits
  • Recombinant Proteins
  • Sodium Channels
  • Protein Serine-Threonine Kinases
  • AMP-Activated Protein Kinases
  • PRKAA1 protein, human