Regulation of KATP Channel Trafficking in Pancreatic β-Cells by Protein Histidine Phosphorylation

Diabetes. 2018 May;67(5):849-860. doi: 10.2337/db17-1433. Epub 2018 Feb 12.

Abstract

Protein histidine phosphatase 1 (PHPT-1) is an evolutionarily conserved 14-kDa protein that dephosphorylates phosphohistidine. PHPT-1-/- mice were generated to gain insight into the role of PHPT-1 and histidine phosphorylation/dephosphorylation in mammalian biology. PHPT-1-/- mice exhibited neonatal hyperinsulinemic hypoglycemia due to impaired trafficking of KATP channels to the plasma membrane in pancreatic β-cells in response to low glucose and leptin and resembled patients with congenital hyperinsulinism (CHI). The defect in KATP channel trafficking in PHPT-1-/- β-cells was due to the failure of PHPT-1 to directly activate transient receptor potential channel 4 (TRPC4), resulting in decreased Ca2+ influx and impaired downstream activation of AMPK. Thus, these studies demonstrate a critical role for PHPT-1 in normal pancreatic β-cell function and raise the possibility that mutations in PHPT-1 and/or TRPC4 may account for yet to be defined cases of CHI.

Publication types

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

MeSH terms

  • Animals
  • Animals, Newborn
  • Calcium / metabolism
  • Congenital Hyperinsulinism / genetics
  • Congenital Hyperinsulinism / metabolism
  • Disease Models, Animal
  • Histidine / metabolism*
  • Hyperinsulinism / genetics*
  • Hyperinsulinism / metabolism
  • Hypoglycemia / genetics*
  • Hypoglycemia / metabolism
  • Insulin-Secreting Cells / metabolism*
  • KATP Channels / metabolism*
  • Mice
  • Mice, Knockout
  • Patch-Clamp Techniques
  • Phosphoric Monoester Hydrolases / genetics*
  • Phosphoric Monoester Hydrolases / metabolism
  • Phosphorylation / genetics
  • Protein Transport / genetics*
  • TRPC Cation Channels / metabolism

Substances

  • KATP Channels
  • TRPC Cation Channels
  • TRPC4 ion channel
  • Histidine
  • PHPT1 protein, mouse
  • Phosphoric Monoester Hydrolases
  • Calcium