Identification of phosphopeptide ligands for the Src-homology 2 (SH2) domain of Grb2 by phage display

Eur J Biochem. 1997 Jun 15;246(3):633-7. doi: 10.1111/j.1432-1033.1997.00633.x.

Abstract

We report here on the identification of phosphopetide ligands which interact with the Src-homology 2 (SH2) domain of the adapter protein Grb2 by screening a random peptide library established on phage. Phage were phosphorylated in vitro at an invariant tyrosine residue by a mixture of phosphotyrosine kinases c-Src, Blk and Syk. Selection of binding motifs was carried out by interaction of the library with the recombinant SH2 domain of Grb2 expressed as a glutathione S-transferase (GST) fusion protein. Several subsequent cycles of selection led to the enrichment of phage which bound to the GST-Grb2 SH2 domain only when previously phosphorylated. Sequence analysis revealed that all of the selected phage displayed peptides with the consensus motif Y*M/ENW (Y* denotes phosphotyrosine). One of these peptides, bearing the Y*ENW motif, bound the Grb2 SH2 domain with a threefold higher affinity than the peptide motif Y*VNV derived from the natural ligand Shc. Thus, phage display can be employed to rapidly identify high affinity ligands to SH2 domains.

MeSH terms

  • Adaptor Proteins, Signal Transducing*
  • Amino Acid Sequence
  • Bacteriophage M13
  • Binding, Competitive
  • Biosensing Techniques
  • GRB2 Adaptor Protein
  • Glutathione Transferase / genetics
  • Glutathione Transferase / metabolism
  • Humans
  • Ligands
  • Molecular Sequence Data
  • Peptide Library*
  • Phosphopeptides / metabolism*
  • Proteins / metabolism*
  • Recombinant Fusion Proteins
  • src Homology Domains*

Substances

  • Adaptor Proteins, Signal Transducing
  • GRB2 Adaptor Protein
  • GRB2 protein, human
  • Ligands
  • Peptide Library
  • Phosphopeptides
  • Proteins
  • Recombinant Fusion Proteins
  • Glutathione Transferase