Cardiac RKIP induces a beneficial β-adrenoceptor-dependent positive inotropy

Nat Med. 2015 Nov;21(11):1298-306. doi: 10.1038/nm.3972. Epub 2015 Oct 19.

Abstract

In heart failure therapy, it is generally assumed that attempts to produce a long-term increase in cardiac contractile force are almost always accompanied by structural and functional damage. Here we show that modest overexpression of the Raf kinase inhibitor protein (RKIP), encoded by Pebp1 in mice, produces a well-tolerated, persistent increase in cardiac contractility that is mediated by the β1-adrenoceptor (β1AR). This result is unexpected, as β1AR activation, a major driver of cardiac contractility, usually has long-term adverse effects. RKIP overexpression achieves this tolerance via simultaneous activation of the β2AR subtype. Analogously, RKIP deficiency exaggerates pressure overload-induced cardiac failure. We find that RKIP expression is upregulated in mouse and human heart failure, indicative of an adaptive role for RKIP. Pebp1 gene transfer in a mouse model of heart failure has beneficial effects, suggesting a new therapeutic strategy for heart failure therapy.

Publication types

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

MeSH terms

  • Animals
  • Chromatin Immunoprecipitation
  • Electrophoresis, Gel, Two-Dimensional
  • Gene Knock-In Techniques
  • Gene Knockdown Techniques
  • Gene Transfer Techniques
  • Heart Failure / genetics*
  • Heart Failure / metabolism
  • Humans
  • Immunohistochemistry
  • In Situ Nick-End Labeling
  • Mice
  • Mice, Transgenic
  • Myocardial Contraction / genetics*
  • Myocytes, Cardiac / metabolism*
  • Phosphatidylethanolamine Binding Protein / genetics*
  • Phosphatidylethanolamine Binding Protein / metabolism
  • Receptors, Adrenergic, beta-1 / metabolism*
  • Reverse Transcriptase Polymerase Chain Reaction

Substances

  • PEBP1 protein, human
  • PEBP1 protein, rat
  • Phosphatidylethanolamine Binding Protein
  • Raf kinase inhibitory protein, mouse
  • Receptors, Adrenergic, beta-1