Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands

J Biol Chem. 2007 Mar 30;282(13):9657-9665. doi: 10.1074/jbc.M610461200. Epub 2007 Jan 23.

Abstract

Data relating to the structural basis of ligand recognition by integrins are limited. Here we describe the physical requirements for high affinity binding of ligands to alpha v beta6. By combining a series of structural analyses with functional testing, we show that 20-mer peptide ligands, derived from high affinity ligands of alpha v beta6 (foot-and-mouth-disease virus, latency associated peptide), have a common structure comprising an Arg-Gly-Asp motif at the tip of a hairpin turn followed immediately by a C-terminal helix. This arrangement allows two conserved Leu/Ile residues at Asp(+1) and Asp(+4) to be presented on the outside face of the helix enabling a potential hydrophobic interaction with the alpha v beta6 integrin, in addition to the Arg-Gly-Asp interaction. The extent of the helix determines peptide affinity for alpha v beta6 and potency as an alpha v beta6 antagonist. A major role of this C-terminal helix is likely to be the correct positioning of the Asp(+1) and Asp(+4) residues. These data suggest an explanation for several biological functions of alpha v beta6 and provide a structural platform for design of alpha v beta6 antagonists.

MeSH terms

  • Amino Acid Motifs / physiology*
  • Amino Acid Sequence
  • Animals
  • Antigens, Neoplasm / chemistry
  • Antigens, Neoplasm / metabolism*
  • CHO Cells
  • Cell Line, Tumor
  • Cricetinae
  • Cricetulus
  • Humans
  • Integrins / chemistry
  • Integrins / metabolism*
  • Ligands
  • Mice
  • Molecular Sequence Data
  • NIH 3T3 Cells
  • Oligopeptides / chemistry
  • Oligopeptides / metabolism
  • Oligopeptides / physiology*
  • Peptide Fragments / chemistry*
  • Peptide Fragments / genetics
  • Peptide Fragments / metabolism*
  • Protein Structure, Secondary
  • Structure-Activity Relationship

Substances

  • Antigens, Neoplasm
  • Integrins
  • Ligands
  • Oligopeptides
  • Peptide Fragments
  • integrin alphavbeta6
  • arginyl-glycyl-aspartic acid