Endorepellin, a novel inhibitor of angiogenesis derived from the C terminus of perlecan

J Biol Chem. 2003 Feb 7;278(6):4238-49. doi: 10.1074/jbc.M210445200. Epub 2002 Nov 14.

Abstract

Perlecan, a ubiquitous basement membrane heparan sulfate proteoglycan, plays key roles in blood vessel growth and structural integrity. We discovered that the C terminus of perlecan potently inhibited four aspects of angiogenesis: endothelial cell migration, collagen-induced endothelial tube morphogenesis, and blood vessel growth in the chorioallantoic membrane and in Matrigel plug assays. The C terminus of perlecan was active at nanomolar concentrations and blocked endothelial cell adhesion to fibronectin and type I collagen, without directly binding to either protein; henceforth we have named it "endorepellin." We also found that endothelial cells possess a significant number of high affinity (K(d) of 11 nm) binding sites for endorepellin and that endorepellin binds endostatin and counteracts its anti-angiogenic effects. Thus, endorepellin represents a novel anti-angiogenic product, which may retard tumor neovascularization and hence tumor growth in vivo.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Angiogenesis Inhibitors / pharmacology*
  • Base Sequence
  • Cell Line
  • Collagen / pharmacology
  • Collagen Type XVIII
  • DNA Primers
  • Endostatins
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Heparan Sulfate Proteoglycans / chemistry*
  • Heparan Sulfate Proteoglycans / isolation & purification
  • Heparan Sulfate Proteoglycans / pharmacology*
  • Humans
  • Peptide Fragments / chemistry
  • Peptide Fragments / isolation & purification
  • Peptide Fragments / pharmacology*
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / pharmacology

Substances

  • Angiogenesis Inhibitors
  • Collagen Type XVIII
  • DNA Primers
  • Endostatins
  • Heparan Sulfate Proteoglycans
  • Peptide Fragments
  • Recombinant Proteins
  • perlecan
  • Collagen