Fibroblast growth factor receptor signalling is dictated by specific heparan sulphate saccharides

Curr Biol. 1999 Nov 18;9(22):1343-6. doi: 10.1016/s0960-9822(00)80060-3.

Abstract

Signalling by fibroblast growth factors (FGFs) through FGF receptors (FGFRs) depends on the cell-surface polysaccharide heparan sulphate (HS) [1] [2]. HS has an ordered domain structure of highly diverse saccharide motifs that present unique displays of sulphate, carboxyl and hydroxyl groups [3]. These motifs interact with many proteins, particularly growth factors. HS binds both to FGFs [4] [5] [6] and FGFRs [7], and probably activates signalling by facilitating ligand-induced receptor dimerisation [8] [9]. Nevertheless, the extent to which specific HS saccharide sequences play a regulatory role has not been established. By screening a library of structurally diverse HS decasaccharides in bioassays of FGF signalling mediated by three different FGFR isoforms, we found that saccharides showed specificity for both ligands and receptors; some saccharides selectively activated FGF signalling through different FGFR isoforms, others acted as negative regulators. We conclude that HS saccharides play critical roles in dictating the specificity of ligand-receptor interactions in FGFR signalling. Controlled alterations in HS structures [10] would provide a mechanism for regulation of cellular responsiveness to growth factors that bind HS.

Publication types

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

MeSH terms

  • Animals
  • Combinatorial Chemistry Techniques
  • Dimerization
  • Fibroblast Growth Factors / physiology*
  • Hematopoietic Stem Cells / metabolism
  • Heparin / metabolism
  • Heparitin Sulfate / physiology*
  • Ligands
  • Mice
  • Oligosaccharides / isolation & purification
  • Oligosaccharides / metabolism*
  • Polysaccharide-Lyases / metabolism
  • Protein Binding
  • Receptors, Fibroblast Growth Factor / physiology*
  • Signal Transduction / physiology*
  • Structure-Activity Relationship
  • Substrate Specificity
  • Swine

Substances

  • Ligands
  • Oligosaccharides
  • Receptors, Fibroblast Growth Factor
  • Fibroblast Growth Factors
  • Heparin
  • Heparitin Sulfate
  • Polysaccharide-Lyases
  • heparitinsulfate lyase