The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues

D. Gomika Udugamasooriya, Geoff Dunham, Caroline Ritchie, Rolf A. Brekken, Thomas Kodadek

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.

Original languageEnglish (US)
Pages (from-to)5892-5894
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number22
DOIs
StatePublished - Nov 15 2008

Keywords

  • Glycine scan
  • Minimum pharmacophore
  • Peptoid
  • Sarcosine scan

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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