A peptoid "antibody surrogate" that antagonizes VEGF receptor 2 activity

J Am Chem Soc. 2008 Apr 30;130(17):5744-52. doi: 10.1021/ja711193x. Epub 2008 Apr 2.


We report a two-color, cell-based screen to identify specific receptor-binding compounds in a combinatorial library of peptoids displayed on beads. We apply this strategy to the isolation of vascular endothelial growth factor receptor 2 (VEGFR2)-binding peptoids. A dimeric derivative of one of these lead compounds is shown to be an antagonist of VEGFR2 activity both in vitro and in vivo. This methodology provides a potentially general route to synthetic molecules that bind integral membrane receptors with affinities and specificities similar to those of antibodies, but which are far smaller and easier to make and manipulate.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry
  • Antibodies, Monoclonal / immunology*
  • Antibodies, Monoclonal / isolation & purification
  • Binding Sites
  • Cell Membrane / chemistry
  • Cell Membrane / metabolism
  • Cells, Cultured
  • Chromatography, High Pressure Liquid
  • Dimerization
  • Humans
  • Immunohistochemistry
  • Ligands
  • Peptoids / chemistry
  • Peptoids / immunology*
  • Peptoids / isolation & purification*
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*
  • Vascular Endothelial Growth Factor Receptor-2 / chemistry
  • Vascular Endothelial Growth Factor Receptor-2 / metabolism


  • Antibodies, Monoclonal
  • Ligands
  • Peptoids
  • Vascular Endothelial Growth Factor Receptor-2