Structural basis for specificity switching of the Src SH2 domain

Mol Cell. 2000 Jun;5(6):1043-9. doi: 10.1016/s1097-2765(00)80269-5.

Abstract

The Src SH2 domain binds pYEEI-containing phosphopeptides in an extended conformation with a hydrophobic pocket, which includes ThrEF1, binding Ile(pY +3). Mutating ThrEF1 to tryptophan switches specificity to an Asn(pY +2) requirement, yielding a biological mimic of the Grb2 SH2 domain. Here we show that the Src ThrEF1Trp SH2 domain mutant binds pYVNV phosphopeptides in a beta turn conformation, which, despite differing conformations of the interacting tryptophan, closely resembles the native Grb2/pYVNV cognate peptide binding mode. The ThrEF1Trp substitution therefore switches specificity by physically occluding the pTyr +3 binding pocket and by providing additional interaction surface area for Asn(pY +2). This demonstrates structurally how novel SH2 domain specificities may rapidly evolve through single amino acid substitutions and suggests how new signaling pathways may develop.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing*
  • Amino Acid Sequence
  • Amino Acid Substitution
  • Animals
  • Binding Sites
  • CSK Tyrosine-Protein Kinase
  • Chickens*
  • Crystallography, X-Ray
  • Evolution, Molecular
  • GRB2 Adaptor Protein
  • Ligands
  • Models, Molecular
  • Mutation
  • Phosphopeptides / chemistry
  • Phosphopeptides / metabolism*
  • Protein Binding
  • Protein Conformation
  • Protein-Tyrosine Kinases / chemistry*
  • Protein-Tyrosine Kinases / genetics
  • Protein-Tyrosine Kinases / metabolism*
  • Proteins / chemistry
  • Proteins / metabolism
  • Signal Transduction / genetics
  • Substrate Specificity
  • src Homology Domains* / genetics
  • src-Family Kinases

Substances

  • Adaptor Proteins, Signal Transducing
  • GRB2 Adaptor Protein
  • Ligands
  • Phosphopeptides
  • Proteins
  • Protein-Tyrosine Kinases
  • CSK Tyrosine-Protein Kinase
  • src-Family Kinases

Associated data

  • PDB/1F1W
  • PDB/1F2F