Peroxisomal proliferator-activated receptor-gamma upregulates glucokinase gene expression in beta-cells

Diabetes. 2002 Mar;51(3):676-85. doi: 10.2337/diabetes.51.3.676.

Abstract

Thiazolidinediones, synthetic ligands of peroxisomal proliferator-activated receptor-gamma (PPAR-gamma), improve peripheral insulin sensitivity and glucose-stimulated insulin secretion in pancreatic beta-cells. To explore the role of PPAR-gamma in glucose sensing of beta-cells, we have dissected the beta-cell-specific glucokinase (betaGK) promoter, which constitutes glucose-sensing apparatus in pancreatic beta-cells, and identified a peroxisomal proliferator response element (PPRE) in the promoter. The betaGK-PPRE is located in the region between +47 and +68 bp. PPAR-gamma/retinoid X receptor-alpha heterodimer binds to the element and activates the betaGK promoter. The betaGK promoter lacking or having mutations in PPRE cannot be activated by PPAR-gamma. PPAR-gamma activates the betaGK promoter in beta-cells as well as non-beta-cells. Furthermore, troglitazone increases endogenous GK expression and its enzyme activity in beta-cell lines. These results indicate that PPAR-gamma can regulate GK expression in beta-cells. Taking these results together with our previous work, we conclude that PPAR-gamma regulates gene expression of glucose-sensing apparatus and thereby improves glucose-sensing ability of beta-cells, contributing to the restoration of beta-cell function in type 2 diabetic subjects by troglitazone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Chromans / pharmacology
  • DNA / metabolism
  • Dimerization
  • Enzyme Activation / drug effects
  • Gene Expression / drug effects
  • Glucokinase / genetics*
  • Hypoglycemic Agents / pharmacology
  • Islets of Langerhans / enzymology*
  • Mice
  • Mutagenesis, Site-Directed
  • Promoter Regions, Genetic
  • Rats
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Receptors, Retinoic Acid / metabolism
  • Response Elements
  • Retinoid X Receptors
  • Thiazoles / pharmacology
  • Thiazolidinediones*
  • Transcription Factors / metabolism
  • Transcription Factors / pharmacology
  • Transcription Factors / physiology*
  • Transcriptional Activation
  • Transfection
  • Troglitazone

Substances

  • Chromans
  • Hypoglycemic Agents
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Retinoic Acid
  • Retinoid X Receptors
  • Thiazoles
  • Thiazolidinediones
  • Transcription Factors
  • DNA
  • Glucokinase
  • Troglitazone