Type I interferons mediate pancreatic toxicities of PERK inhibition

Proc Natl Acad Sci U S A. 2015 Dec 15;112(50):15420-5. doi: 10.1073/pnas.1516362112. Epub 2015 Dec 1.

Abstract

The great preclinical promise of the pancreatic endoplasmic reticulum kinase (PERK) inhibitors in neurodegenerative disorders and cancers is marred by pancreatic injury and diabetic syndrome observed in PERK knockout mice and humans lacking PERK function and suffering from Wolcott-Rallison syndrome. PERK mediates many of the unfolded protein response (UPR)-induced events, including degradation of the type 1 interferon (IFN) receptor IFNAR1 in vitro. Here we report that whole-body or pancreas-specific Perk ablation in mice leads to an increase in IFNAR1 protein levels and signaling in pancreatic tissues. Concurrent IFNAR1 deletion attenuated the loss of PERK-deficient exocrine and endocrine pancreatic tissues and prevented the development of diabetes. Experiments using pancreas-specific Perk knockouts, bone marrow transplantation, and cultured pancreatic islets demonstrated that stabilization of IFNAR1 and the ensuing increased IFN signaling in pancreatic tissues represents a major driver of injury triggered by Perk loss. Neutralization of IFNAR1 prevented pancreatic toxicity of PERK inhibitor, indicating that blocking the IFN pathway can mitigate human genetic disorders associated with PERK deficiency and help the clinical use of PERK inhibitors.

Keywords: PERK; Wolcott-Rallison syndrome; diabetes; interferon; pancreas.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Caspase 3 / metabolism
  • Diabetes Mellitus, Experimental / enzymology
  • Diabetes Mellitus, Experimental / pathology
  • Down-Regulation / drug effects
  • Endoplasmic Reticulum / drug effects
  • Endoplasmic Reticulum / metabolism
  • Enzyme Activation / drug effects
  • Fluorescent Antibody Technique
  • Interferon Type I / metabolism*
  • Islets of Langerhans / drug effects
  • Islets of Langerhans / metabolism
  • Mice
  • Pancreas / drug effects
  • Pancreas / enzymology*
  • Pancreas / pathology*
  • Protein Kinase Inhibitors / toxicity
  • Receptor, Interferon alpha-beta / metabolism*
  • Signal Transduction / drug effects
  • Unfolded Protein Response
  • Up-Regulation / drug effects
  • eIF-2 Kinase / antagonists & inhibitors*
  • eIF-2 Kinase / metabolism

Substances

  • Ifnar1 protein, mouse
  • Interferon Type I
  • Protein Kinase Inhibitors
  • Receptor, Interferon alpha-beta
  • PERK kinase
  • eIF-2 Kinase
  • Caspase 3