Pathological role of serum- and glucocorticoid-regulated kinase 1 in adverse ventricular remodeling

Circulation. 2012 Oct 30;126(18):2208-19. doi: 10.1161/CIRCULATIONAHA.112.115592. Epub 2012 Sep 26.

Abstract

Background: Heart failure is a growing cause of morbidity and mortality. Cardiac phosphatidylinositol 3-kinase signaling promotes cardiomyocyte survival and function, but it is paradoxically activated in heart failure, suggesting that chronic activation of this pathway may become maladaptive. Here, we investigated the downstream phosphatidylinositol 3-kinase effector, serum- and glucocorticoid-regulated kinase-1 (SGK1), in heart failure and its complications.

Methods and results: We found that cardiac SGK1 is activated in human and murine heart failure. We investigated the role of SGK1 in the heart by using cardiac-specific expression of constitutively active or dominant-negative SGK1. Cardiac-specific activation of SGK1 in mice increased mortality, cardiac dysfunction, and ventricular arrhythmias. The proarrhythmic effects of SGK1 were linked to biochemical and functional changes in the cardiac sodium channel and could be reversed by treatment with ranolazine, a blocker of the late sodium current. Conversely, cardiac-specific inhibition of SGK1 protected mice after hemodynamic stress from fibrosis, heart failure, and sodium channel alterations.

Conclusions: SGK1 appears both necessary and sufficient for key features of adverse ventricular remodeling and may provide a novel therapeutic target in cardiac disease.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetanilides / therapeutic use
  • Animals
  • Cardiomegaly, Exercise-Induced
  • Cardiomyopathy, Dilated / enzymology*
  • Consensus Sequence
  • Disease Models, Animal
  • Electrocardiography
  • Enzyme Induction
  • Heart Failure / enzymology*
  • Humans
  • Hypertension / complications
  • Immediate-Early Proteins / chemistry
  • Immediate-Early Proteins / deficiency
  • Immediate-Early Proteins / genetics
  • Immediate-Early Proteins / metabolism
  • Immediate-Early Proteins / physiology*
  • Ion Channel Gating / drug effects
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • NAV1.5 Voltage-Gated Sodium Channel / chemistry
  • NAV1.5 Voltage-Gated Sodium Channel / drug effects
  • NAV1.5 Voltage-Gated Sodium Channel / physiology
  • Phosphatidylinositol 3-Kinases / physiology
  • Phosphorylation
  • Piperazines / therapeutic use
  • Protein Interaction Mapping
  • Protein Processing, Post-Translational
  • Protein Serine-Threonine Kinases / chemistry
  • Protein Serine-Threonine Kinases / deficiency
  • Protein Serine-Threonine Kinases / genetics
  • Protein Serine-Threonine Kinases / metabolism
  • Protein Serine-Threonine Kinases / physiology*
  • Ranolazine
  • Sodium Channel Blockers / pharmacology
  • Sodium Channel Blockers / therapeutic use
  • Tachycardia, Ventricular / enzymology
  • Tachycardia, Ventricular / etiology
  • Ventricular Remodeling / physiology*

Substances

  • Acetanilides
  • Immediate-Early Proteins
  • NAV1.5 Voltage-Gated Sodium Channel
  • Piperazines
  • Scn5a protein, mouse
  • Sodium Channel Blockers
  • Ranolazine
  • Protein Serine-Threonine Kinases
  • serum-glucocorticoid regulated kinase