Novel arguments in favor of the substrate-transport model of glucose-6-phosphatase

Diabetes. 2001 Jul;50(7):1531-8. doi: 10.2337/diabetes.50.7.1531.

Abstract

The purpose of this work was to discriminate between two models for glucose-6-phosphatase: one in which the enzyme has its catalytic site oriented toward the lumen of the endoplasmic reticulum, requiring transporters for glucose-6-phosphate, inorganic phosphate (Pi), and glucose (substrate-transport model), and a second one in which the hydrolysis of glucose-6-phosphate occurs inside the membrane (conformational model). We show that microsomes preloaded with yeast phosphoglucose isomerase catalyzed the detritiation of [2-(3)H]glucose-6-phosphate and that this reaction was inhibited by up to 90% by S3483, a compound known to inhibit glucose-6-phosphate hydrolysis in intact but not in detergent-treated microsomes. These results indicate that glucose-6-phosphate is transported to the lumen of the microsomes in an S3483-sensitive manner. Detritiation by intramicrosomal phosphoglucose isomerase was stimulated twofold by 1 mmol/l vanadate, a phosphatase inhibitor, indicating that glucose-6-phosphatase and the isomerase compete for the same intravesicular pool of glucose-6-phosphate. To investigate the site of release of Pi from glucose-6-phosphate, we incubated microsomes with Pb(2+), which forms an insoluble complex with Pi, preventing its rapid exit from the microsomes. Under these conditions, approximately 80% of the Pi that was formed after 5 min was intramicrosomal, compared with <10% in the absence of Pb(2+). We also show that, when incubated with glucose-6-phosphate and mannitol, glucose-6-phosphatase formed mannitol-1-phosphate and that this nonphysiological product was initially present within the microsomes before being released to the medium. These results indicate that the primary site of product release by glucose-6-phosphatase is the lumen of the endoplasmic reticulum.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport, Active
  • Catalytic Domain
  • Cells, Cultured
  • Cyclohexanecarboxylic Acids / pharmacology
  • Endoplasmic Reticulum / enzymology
  • Glucose-6-Phosphatase / metabolism*
  • Glucose-6-Phosphate Isomerase / metabolism
  • Hydrolysis
  • Male
  • Microsomes, Liver / enzymology
  • Models, Chemical*
  • Phosphates / metabolism
  • Protein Conformation
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship

Substances

  • Cyclohexanecarboxylic Acids
  • Phosphates
  • S 3483
  • Glucose-6-Phosphatase
  • Glucose-6-Phosphate Isomerase