In vitro evaluation of synthetic heparin-like conjugates comprising different thrombin binding domains

Bioorg Med Chem Lett. 1998 May 19;8(10):1201-6. doi: 10.1016/s0960-894x(98)00196-6.

Abstract

The syntheses of several heparin-like glycoconjugates (i.e., 16a-f) containing identical AT III binding domains (ABD) and spacers but different thrombin binding domains (TBDs) are described. Biological activities of conjugates 16a-f indicate that the thrombin inhibitory activity is mainly determined by the charge density of the TBD moiety.

MeSH terms

  • Angiotensin III / metabolism
  • Binding Sites
  • Carbohydrate Conformation
  • Carbohydrate Sequence
  • Dermatan Sulfate / chemistry
  • Drug Design
  • Glycoconjugates / chemical synthesis*
  • Glycoconjugates / chemistry
  • Glycoconjugates / pharmacology*
  • Heparin / analogs & derivatives*
  • Heparin / pharmacology*
  • Models, Molecular
  • Molecular Sequence Data
  • Oligosaccharides / chemical synthesis*
  • Oligosaccharides / chemistry
  • Oligosaccharides / pharmacology
  • Structure-Activity Relationship
  • Thrombin / metabolism*

Substances

  • Glycoconjugates
  • Oligosaccharides
  • Angiotensin III
  • Dermatan Sulfate
  • Heparin
  • Thrombin