Inactivation of the Glucose-Dependent Insulinotropic Polypeptide Receptor Improves Outcomes following Experimental Myocardial Infarction

Cell Metab. 2018 Feb 6;27(2):450-460.e6. doi: 10.1016/j.cmet.2017.11.003. Epub 2017 Dec 21.

Abstract

Incretin hormones exert pleiotropic metabolic actions beyond the pancreas. Although the heart expresses both incretin receptors, the cardiac biology of GIP receptor (GIPR) action remains incompletely understood. Here we show that GIPR agonism did not impair the response to cardiac ischemia. In contrast, genetic elimination of the Gipr reduced myocardial infarction (MI)-induced ventricular injury and enhanced survival associated with reduced hormone sensitive lipase (HSL) phosphorylation; it also increased myocardial triacylglycerol (TAG) stores. Conversely, direct GIPR agonism in the isolated heart reduced myocardial TAG stores and increased fatty acid oxidation. The cardioprotective phenotype in Gipr-/- mice was partially reversed by pharmacological activation or genetic overexpression of HSL. Selective Gipr inactivation in cardiomyocytes phenocopied Gipr-/- mice, resulting in improved survival and reduced adverse remodeling following experimental MI. Hence, the cardiomyocyte GIPR regulates fatty acid metabolism and the adaptive response to ischemic cardiac injury. These findings have translational relevance for developing GIPR-based therapeutics.

Keywords: G-protein-coupled receptor; cardiovascular; diabetes; glucose-dependent insulinotropic polypeptide; gut peptide; hormone sensitive lipase; incretin; ischemia; myocardial infarction; obesity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Enzyme Activation
  • Gastric Inhibitory Polypeptide / metabolism
  • HEK293 Cells
  • Heart Failure / pathology
  • Humans
  • MAP Kinase Signaling System
  • Mice
  • Mice, Inbred C57BL
  • Myocardial Infarction / diagnostic imaging
  • Myocardial Infarction / pathology*
  • Myocardial Infarction / physiopathology
  • Myocardial Infarction / prevention & control
  • Myocardium / metabolism
  • Myocardium / pathology
  • Myocytes, Cardiac / metabolism
  • Phosphorylation
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Receptors, Gastrointestinal Hormone / deficiency
  • Receptors, Gastrointestinal Hormone / genetics
  • Receptors, Gastrointestinal Hormone / metabolism*
  • Signal Transduction
  • Sterol Esterase / metabolism
  • Triglycerides / metabolism
  • Ventricular Remodeling

Substances

  • RNA, Messenger
  • Receptors, Gastrointestinal Hormone
  • Triglycerides
  • Gastric Inhibitory Polypeptide
  • gastric inhibitory polypeptide receptor
  • Sterol Esterase
  • Adenylyl Cyclases