G6PC2 controls glucagon secretion by defining the set point for glucose in pancreatic α cells

Sci Transl Med. 2025 Jan;17(779):eadi6148. doi: 10.1126/scitranslmed.adi6148. Epub 2025 Jan 1.

Abstract

Elevated glucagon concentrations have been reported in patients with type 2 diabetes (T2D). A critical role for α cell-intrinsic mechanisms in regulating glucagon secretion was previously established through genetic manipulation of the glycolytic enzyme glucokinase (GCK) in mice. Genetic variation at the glucose-6-phosphatase catalytic subunit 2 (G6PC2) locus, encoding an enzyme that opposes GCK, has been reproducibly associated with fasting blood glucose and hemoglobin A1c. Here, we found that trait-associated variants in the G6PC2 promoter are located in open chromatin not just in β but also in α cells and documented allele-specific G6PC2 expression of linked variants in human α cells. Using α cell-specific gene ablation of G6pc2 in mice, we showed that this gene plays a critical role in controlling glucose suppression of amino acid-stimulated glucagon secretion independent of alterations in insulin output, islet hormone content, or islet morphology, findings that we confirmed in primary human α cells. Collectively, our data demonstrate that G6PC2 affects glycemic control via its action in α cells and possibly suggest that G6PC2 inhibitors might help control blood glucose through a bihormonal mechanism.

MeSH terms

  • Animals
  • Glucagon* / metabolism
  • Glucagon-Secreting Cells* / metabolism
  • Glucose* / metabolism
  • Glucose-6-Phosphatase* / metabolism
  • Humans
  • Mice
  • Promoter Regions, Genetic / genetics

Substances

  • Glucagon
  • Glucose-6-Phosphatase
  • Glucose
  • G6PC2 protein, human
  • G6pc2 protein, mouse