KRas induces a Src/PEAK1/ErbB2 kinase amplification loop that drives metastatic growth and therapy resistance in pancreatic cancer

Cancer Res. 2012 May 15;72(10):2554-64. doi: 10.1158/0008-5472.CAN-11-3552.

Abstract

Early biomarkers and effective therapeutic strategies are desperately needed to treat pancreatic ductal adenocarcinoma (PDAC), which has a dismal 5-year patient survival rate. Here, we report that the novel tyrosine kinase PEAK1 is upregulated in human malignancies, including human PDACs and pancreatic intraepithelial neoplasia (PanIN). Oncogenic KRas induced a PEAK1-dependent kinase amplification loop between Src, PEAK1, and ErbB2 to drive PDAC tumor growth and metastasis in vivo. Surprisingly, blockade of ErbB2 expression increased Src-dependent PEAK1 expression, PEAK1-dependent Src activation, and tumor growth in vivo, suggesting a mechanism for the observed resistance of patients with PDACs to therapeutic intervention. Importantly, PEAK1 inactivation sensitized PDAC cells to trastuzumab and gemcitabine therapy. Our findings, therefore, suggest that PEAK1 is a novel biomarker, critical signaling hub, and new therapeutic target in PDACs.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Biomarkers, Tumor / analysis
  • Carcinoma, Pancreatic Ductal / genetics*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Genes, erbB-2*
  • Genes, ras
  • Humans
  • Mice
  • Mice, Transgenic
  • Models, Molecular
  • Neoplasm Metastasis / genetics
  • Neoplasm Transplantation
  • Oncogene Protein pp60(v-src) / genetics*
  • Pancreatic Neoplasms / genetics*
  • Protein-Tyrosine Kinases / genetics*
  • Signal Transduction / genetics
  • Transcriptional Activation
  • Up-Regulation

Substances

  • Biomarkers, Tumor
  • SRC protein, Rous sarcoma virus
  • PEAK1 protein, human
  • Protein-Tyrosine Kinases
  • Oncogene Protein pp60(v-src)