Synthesis and evaluation of fructose analogues as inhibitors of the D-fructose transporter GLUT5

Bioorg Med Chem. 2000 Jul;8(7):1825-33. doi: 10.1016/s0968-0896(00)00108-5.

Abstract

We have examined the specificity and binding-site spatial requirements of the fructose transporter GLUT5. Interaction with a series of fructofuranosides and fructopyranosides suggests that both furanose and pyranose ring forms of D-fructose combine with GLUT5. The epimers of D-fructose all have low affinity for GLUT5 suggesting that the transporter requires all hydroxyls to be in the fructo-configuration. Similarly there is poor tolerance of all allyl derivatives of D-fructose except 6-O-allyl-D-fructofuranose. Therefore, the C-6 position offers the most suitable position for development of affinity probes and labels for exploring GLUT5 biochemistry.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport / drug effects
  • CHO Cells
  • Carbon Radioisotopes
  • Cricetinae
  • Fructose / analogs & derivatives*
  • Fructose / chemical synthesis
  • Fructose / pharmacokinetics*
  • Glucose Transporter Type 5
  • Kinetics
  • Molecular Structure
  • Monosaccharide Transport Proteins / antagonists & inhibitors*
  • Monosaccharide Transport Proteins / metabolism
  • Structure-Activity Relationship

Substances

  • Carbon Radioisotopes
  • Glucose Transporter Type 5
  • Monosaccharide Transport Proteins
  • Fructose