Structural basis for the interaction of a vascular endothelial growth factor mimic peptide motif and its corresponding receptors

Chem Biol. 2005 Oct;12(10):1075-83. doi: 10.1016/j.chembiol.2005.07.008.

Abstract

Vascular endothelial growth factor (VEGF) is central to the survival and development of the vascular and nervous systems. We screened phage display libraries and built a peptide-based ligand-receptor map of binding sites within the VEGF family. We then validated a cyclic peptide, CPQPRPLC, as a VEGF-mimic that binds specifically to neuropilin-1 and VEGF receptor-1. Here, we use NMR spectroscopy to understand the structural basis of the interaction between our mimic peptide and the VEGF receptors. We show that: (1) CPQPRPLC has multiple interactive conformations; (2) receptor binding is mediated by the motif Arg-Pro-Leu; and (3) the Pro residue within Arg-Pro-Leu participates in binding to neuropilin-1 but not to VEGF receptor-1, perhaps representing an evolutionary gain-of-function. Therefore, Arg-Pro-Leu is a differential ligand motif to VEGF receptors and a candidate peptidomimetic lead for VEGF pathway modulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Motifs
  • Binding Sites
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Mimicry*
  • Molecular Structure
  • Neuropilin-1 / metabolism
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / metabolism*
  • Peptides, Cyclic / pharmacology
  • Signal Transduction / drug effects
  • Vascular Endothelial Growth Factor Receptor-1 / metabolism
  • Vascular Endothelial Growth Factors / chemistry*
  • Vascular Endothelial Growth Factors / metabolism*

Substances

  • Peptides, Cyclic
  • Vascular Endothelial Growth Factors
  • Neuropilin-1
  • Vascular Endothelial Growth Factor Receptor-1