Inhibition of the SRC Kinase HCK Impairs STAT3-Dependent Gastric Tumor Growth in Mice

Cancer Immunol Res. 2020 Apr;8(4):428-435. doi: 10.1158/2326-6066.CIR-19-0623. Epub 2020 Jan 28.

Abstract

Persistent activation of the latent transcription factor STAT3 is observed in gastric tumor epithelial and immune cells and is associated with a poor patient prognosis. Although targeting STAT3-activating upstream kinases offers therapeutically viable targets with limited specificity, direct inhibition of STAT3 remains challenging. Here we provide functional evidence that myeloid-specific hematopoietic cell kinase (HCK) activity can drive STAT3-dependent epithelial tumor growth in mice and is associated with alternative macrophage activation alongside matrix remodeling and tumor cell invasion. Accordingly, genetic reduction of HCK expression in bone marrow-derived cells or systemic pharmacologic inhibition of HCK activity suppresses alternative macrophage polarization and epithelial STAT3 activation, and impairs tumor growth. These data validate HCK as a molecular target for the treatment of human solid tumors harboring excessive STAT3 activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Humans
  • Macrophage Activation / drug effects
  • Male
  • Mice
  • Mice, Transgenic
  • Phosphorylation / drug effects
  • Proto-Oncogene Proteins c-hck / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-hck / metabolism
  • Pyrimidines / pharmacology*
  • Pyrroles / pharmacology*
  • STAT3 Transcription Factor / metabolism*
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / metabolism
  • Stomach Neoplasms / pathology
  • Survival Rate

Substances

  • Pyrimidines
  • Pyrroles
  • RK-20449
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Stat3 protein, mouse
  • HCK protein, human
  • Hck protein, mouse
  • Proto-Oncogene Proteins c-hck