Targeting PKCα alleviates iron overload in diabetes and hemochromatosis through the inhibition of ferroportin

Blood. 2024 Sep 26;144(13):1433-1444. doi: 10.1182/blood.2024023829.

Abstract

Ferroportin (Fpn) is the only iron exporter, playing a crucial role in systemic iron homeostasis. Fpn is negatively regulated by its ligand hepcidin, but other potential regulators in physiological and disease conditions remain poorly understood. Diabetes is a metabolic disorder that develops body iron loading with unknown mechanisms. By using diabetic mouse models and human duodenal specimens, we demonstrated that intestinal Fpn expression was increased in diabetes in a hepcidin-independent manner. Protein kinase C (PKC) is hyperactivated in diabetes. We showed that PKCα was required to sustain baseline Fpn expression and diabetes-induced Fpn upregulation in the enterocytes and macrophages. Knockout of PKCα abolished diabetes-associated iron overload. Mechanistically, activation of PKCα increased the exocytotic trafficking of Fpn and decreased the endocytic trafficking of Fpn in the resting state. Hyperactive PKCα also suppressed hepcidin-induced ubiquitination, internalization, and degradation of Fpn. We further observed that iron loading in the enterocytes and macrophages activated PKCα, acting as a novel mechanism to enhance Fpn-dependent iron efflux. Finally, we demonstrated that the loss-of-function of PKCα and pharmacological inhibition of PKC significantly alleviated hereditary hemochromatosis-associated iron overload. Our study has highlighted, to our knowledge, for the first time, that PKCα is an important positive regulator of Fpn and a new target in the control of iron homeostasis.

MeSH terms

  • Animals
  • Cation Transport Proteins* / genetics
  • Cation Transport Proteins* / metabolism
  • Diabetes Mellitus, Experimental / metabolism
  • Enterocytes / metabolism
  • Enterocytes / pathology
  • Hemochromatosis* / genetics
  • Hemochromatosis* / metabolism
  • Hemochromatosis* / pathology
  • Hepcidins* / genetics
  • Hepcidins* / metabolism
  • Humans
  • Iron / metabolism
  • Iron Overload* / metabolism
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Protein Kinase C-alpha* / genetics
  • Protein Kinase C-alpha* / metabolism

Substances

  • metal transporting protein 1
  • Protein Kinase C-alpha
  • Cation Transport Proteins
  • Hepcidins
  • Iron
  • Prkca protein, mouse