The cdk5 kinase regulates the STAT3 transcription factor to prevent DNA damage upon topoisomerase I inhibition

J Biol Chem. 2010 Aug 27;285(35):26765-26778. doi: 10.1074/jbc.M109.092304. Epub 2010 Jun 1.

Abstract

The STAT3 transcription factors are cytoplasmic proteins that induce gene activation in response to growth factor stimulation. Following tyrosine phosphorylation, STAT3 proteins dimerize, translocate to the nucleus, and activate specific target genes involved in cell-cycle progression. Despite its importance in cancer cells, the molecular mechanisms by which this protein is regulated in response to DNA damage remain to be characterized. In this study, we show that STAT3 is activated in response to topoisomerase I inhibition. Following treatment, STAT3 is phosphorylated on its C-terminal serine 727 residue but not on its tyrosine 705 site. We also show that topoisomerase I inhibition induced the up-regulation of the cdk5 kinase, a protein initially described in neuronal stress responses. In co-immunoprecipitations, cdk5 was found to associate with STAT3, and pulldown experiments indicated that it associates with the C-terminal activation domain of STAT3 upon DNA damage. Importantly, the cdk5-STAT3 pathway reduced DNA damage in response to topoisomerase I inhibition through the up-regulation of Eme1, an endonuclease involved in DNA repair. ChIP experiments indicated that STAT3 can be found associated with the Eme1 promoter when phosphorylated only on its serine 727 residue and not on tyrosine 705. We therefore propose that the cdk5-STAT3 oncogenic pathway plays an important role in the expression of DNA repair genes and that these proteins could be used as predictive markers of tumors that will fail to respond to chemotherapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biomarkers, Tumor / genetics
  • Biomarkers, Tumor / metabolism*
  • Cell Line, Tumor
  • Cyclin-Dependent Kinase 5 / genetics
  • Cyclin-Dependent Kinase 5 / metabolism*
  • DNA Damage / drug effects*
  • DNA Topoisomerases, Type I / genetics
  • DNA Topoisomerases, Type I / metabolism*
  • Endodeoxyribonucleases / biosynthesis
  • Endodeoxyribonucleases / genetics
  • Enzyme Inhibitors / pharmacology*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Gene Expression Regulation, Neoplastic / genetics
  • Humans
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / metabolism*
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Neoplasms / metabolism*
  • Phosphorylation / drug effects
  • Phosphorylation / genetics
  • Promoter Regions, Genetic / genetics
  • Protein Multimerization / drug effects
  • Protein Multimerization / genetics
  • Protein Structure, Tertiary
  • STAT3 Transcription Factor / genetics
  • STAT3 Transcription Factor / metabolism*
  • Topoisomerase I Inhibitors*

Substances

  • Biomarkers, Tumor
  • Enzyme Inhibitors
  • Neoplasm Proteins
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Topoisomerase I Inhibitors
  • Cyclin-Dependent Kinase 5
  • CDK5 protein, human
  • Eme1 protein, human
  • Endodeoxyribonucleases
  • DNA Topoisomerases, Type I