The identification and characterization of a STAT5 gene signature in hematologic malignancies

Cancer Biomark. 2015;15(1):79-87. doi: 10.3233/CBM-140434.

Abstract

Background: The JAK-STAT pathway is an important signaling pathway downstream of multiple cytokine and growth factor receptors. Dysregulated JAK-STAT signaling has been implicated in the pathogenesis of multiple human malignancies.

Objective: Given this pivotal role of JAK-STAT dysregulation, it is important to identify patients with an overactive JAK-STAT pathway for possible treatment with JAK inhibitors.

Methods: We developed a gene signature assay to detect overactive JAK-STAT signaling. The cancer cell line encyclopedia and associated gene-expression data were used to correlate the activation status of STAT5 with the induction of a set of STAT5 target genes.

Results: Four target genes were identified (PIM1, CISH, SOCS2, and ID1), the expression of which correlated significantly with pSTAT5 status in 40 hematologic tumor cell lines. In pSTAT5-positive models, the expression of the gene signature genes decreased following ruxolitinib treatment, which corresponded to pSTAT5 downmodulation. In pSTAT5-negative cell lines, neither pSTAT5 modulation nor a change in signature gene expression was observed following ruxolitinib treatment.

Conclusions: The gene signature can potentially be used to stratify or enrich for patient populations with activated JAK-STAT5 signaling that might benefit from treatments targeting JAK-STAT signaling. Furthermore, the 4-gene signature is a predictor of the pharmacodynamic effects of ruxolitinib.

Keywords: JAK-STAT; Ruxolitinib; gene signature; pSTAT5.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Female
  • Hematologic Neoplasms / drug therapy
  • Hematologic Neoplasms / genetics*
  • Hematologic Neoplasms / metabolism*
  • Heterografts
  • Humans
  • Janus Kinases / metabolism
  • Mice
  • Mice, Inbred NOD
  • Mice, SCID
  • Nitriles
  • Pyrazoles / pharmacology
  • Pyrimidines
  • STAT5 Transcription Factor / genetics*
  • STAT5 Transcription Factor / metabolism*
  • Signal Transduction / drug effects

Substances

  • Nitriles
  • Pyrazoles
  • Pyrimidines
  • STAT5 Transcription Factor
  • ruxolitinib
  • Janus Kinases