The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice

Nat Commun. 2014 Dec 9:5:5705. doi: 10.1038/ncomms6705.

Abstract

Heart failure (HF) and atrial fibrillation (AF) share common risk factors, frequently coexist and are associated with high mortality. Treatment of HF with AF represents a major unmet need. Here we show that a small molecule, BGP-15, improves cardiac function and reduces arrhythmic episodes in two independent mouse models, which progressively develop HF and AF. In these models, BGP-15 treatment is associated with increased phosphorylation of the insulin-like growth factor 1 receptor (IGF1R), which is depressed in atrial tissue samples from patients with AF. Cardiac-specific IGF1R transgenic overexpression in mice with HF and AF recapitulates the protection observed with BGP-15. We further demonstrate that BGP-15 and IGF1R can provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70; signalling mediators often defective in the aged and diseased heart. As BGP-15 is safe and well tolerated in humans, this study uncovers a potential therapeutic approach for HF and AF.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Atrial Fibrillation / drug therapy*
  • Caveolin 1 / metabolism
  • Caveolin 3 / metabolism
  • Disease Models, Animal
  • Electrocardiography
  • G(M3) Ganglioside / metabolism
  • HSP70 Heat-Shock Proteins / metabolism
  • Heart Failure / prevention & control*
  • Humans
  • Male
  • Mice
  • Mice, Knockout
  • Mice, Transgenic
  • Microarray Analysis
  • Oximes / chemistry*
  • Phosphatidylinositol 3-Kinases / metabolism
  • Phosphorylation
  • Piperidines / chemistry*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Receptor, IGF Type 1 / metabolism
  • Receptors, Somatomedin / metabolism
  • Risk Factors
  • Signal Transduction
  • Transgenes

Substances

  • Caveolin 1
  • Caveolin 3
  • G(M3) Ganglioside
  • HSP70 Heat-Shock Proteins
  • IGF1R protein, human
  • Oximes
  • Piperidines
  • Receptors, Somatomedin
  • Phosphatidylinositol 3-Kinases
  • Receptor, IGF Type 1
  • Proto-Oncogene Proteins c-akt
  • BGP 15