Rapid identification of phosphopeptide ligands for SH2 domains. Screening of peptide libraries by fluorescence-activated bead sorting

J Biol Chem. 1996 Jul 12;271(28):16500-5.

Abstract

A method for the identification of high-affinity ligands to SH2 domains by fluorescence-activated bead sorting (FABS) was established. Recombinant SH2 domains, expressed as glutathione S-transferase (GST) fusion proteins, were incubated with a phosphotyrosine (Y*)-containing peptide library. 6.4 x 10(5) individual peptides of nine amino acids in length (EPX6Y*X19X7X19X7X6) were each displayed on beads. Phosphopeptide interaction of a given SH2 domain was monitored by binding of fluorescein isothiocyanate-labeled antibodies directed against GST. High-fluorescence beads were isolated by flow cytometric sorting. Subsequent pool sequencing of the selected beads revealed a distinct pattern of phosphotyrosine-containing motifs for each individual SH2 domain: the SH2 domain of the adapter protein Grb2 predominantly selected beads with the sequence Y*ENDP, whereas the C-terminal SH2 domain of the tyrosine kinase Syk selected Y*EELD, each motif representing the most frequently found residues C-terminal to the phosphotyrosine. For deconvolution studies, soluble phosphopeptides comprising variations of the Grb2 motifs were resynthesized and analyzed by surface plasmon resonance.

MeSH terms

  • Amino Acid Sequence
  • Base Sequence
  • Cell Line, Transformed
  • DNA, Complementary
  • Enzyme Precursors / chemistry
  • Enzyme Precursors / metabolism
  • Flow Cytometry
  • Fluorescein-5-isothiocyanate
  • Fluorescence
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Ligands
  • Molecular Sequence Data
  • Phosphopeptides / chemistry
  • Phosphopeptides / metabolism*
  • Protein Binding
  • Protein-Tyrosine Kinases / chemistry
  • Protein-Tyrosine Kinases / metabolism
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Syk Kinase
  • src Homology Domains*

Substances

  • DNA, Complementary
  • Enzyme Precursors
  • Intracellular Signaling Peptides and Proteins
  • Ligands
  • Phosphopeptides
  • Recombinant Fusion Proteins
  • Protein-Tyrosine Kinases
  • SYK protein, human
  • Syk Kinase
  • Fluorescein-5-isothiocyanate