Identification of novel inhibitors of fibroblast growth factor (FGF-2) binding to heparin and endothelial cell survival from a structurally diverse carbohybrid library

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3287-90. doi: 10.1016/s0960-894x(02)00700-x.

Abstract

Inhibitors of FGF-2 binding to a heparin-albumin conjugate were identified by ELISA from a library of glucuronic acid derivatives. These compounds were also inhibitors of endothelial cell survival that is dependant on FGF-2 and heparin or heparan sulfate proteoglycans. The results indicate that these bioactive compounds may prove useful as lead structures for the further development of pharmaceutical agents capable of modulating biological activity of FGF-2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Aorta
  • Cattle
  • Cell Survival / drug effects
  • Combinatorial Chemistry Techniques
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects*
  • Fibroblast Growth Factor 2 / antagonists & inhibitors*
  • Fibroblast Growth Factor 2 / metabolism
  • Glucuronic Acid / chemistry
  • Glucuronic Acid / pharmacology*
  • Heparin / metabolism*
  • Protein Binding / drug effects
  • Structure-Activity Relationship

Substances

  • Angiogenesis Inhibitors
  • Fibroblast Growth Factor 2
  • Glucuronic Acid
  • Heparin