Constitutive activation of STAT5 by a point mutation in the SH2 domain

J Biol Chem. 2000 Aug 11;275(32):24407-13. doi: 10.1074/jbc.M909771199.

Abstract

We previously identified a constitutively active form of STAT (signal transducer and activator of transcription) 5A by polymerase chain reaction-driven random mutagenesis followed by retrovirus-mediated expression screening, which had two point mutations in the DNA-binding and transcriptional activation domains, and was designated STAT5A1*6. STAT5A1*6 showed markedly elevated DNA binding and transactivation activities with stable tyrosine phosphorylation and nuclear accumulation, and conferred autonomous cell growth on interleukin 3-dependent Ba/F3 cells. We now report another constitutively active mutant, STAT5A-N642H which has a single point mutation (N642H) in its SH2 domain, identified using the same strategy as that used to identify STAT5A1*6. STAT5A-N642H showed identical properties to those of STAT5A1*6 both biochemically and biologically. Interestingly the mutation in STAT5A-N642H resulted in restoration of the conserved critical histidine which is involved in the binding of phosphotyrosine in the majority of SH2-containing proteins. Introduction of an additional mutation (Y694F) to STAT5A-N642H, which disrupted critical tyrosine 694 required for dimerization of STAT5, abolished all the activities manifested by the mutant STAT5A-N642H, which indicates that dimerization is required for the activity of STAT5A-N642H as was the case for the wild-type STAT5A. The present findings also show that different mutations rendered STAT5A constitutively active, through a common mechanism, which is similar to that of physiological activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3 Cells
  • Amino Acid Substitution
  • Animals
  • Apoptosis
  • Binding Sites
  • COS Cells
  • Cell Differentiation
  • Cell Division / drug effects
  • Cell Line
  • Cell Nucleus / metabolism
  • DNA-Binding Proteins / chemistry*
  • DNA-Binding Proteins / metabolism*
  • Dimerization
  • Granulocyte-Macrophage Colony-Stimulating Factor / pharmacology
  • Humans
  • Interleukin-3 / pharmacology
  • Mice
  • Milk Proteins*
  • Mutagenesis, Site-Directed
  • Phosphorylation
  • Point Mutation
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • STAT5 Transcription Factor
  • Trans-Activators / chemistry*
  • Trans-Activators / metabolism*
  • Transcriptional Activation
  • Transfection
  • Tumor Cells, Cultured
  • Tumor Suppressor Proteins
  • Tyrosine
  • src Homology Domains

Substances

  • DNA-Binding Proteins
  • Interleukin-3
  • Milk Proteins
  • Recombinant Proteins
  • STAT5 Transcription Factor
  • STAT5A protein, human
  • Stat5a protein, mouse
  • Trans-Activators
  • Tumor Suppressor Proteins
  • Tyrosine
  • Granulocyte-Macrophage Colony-Stimulating Factor