Combined deletion of Pten and p53 in mammary epithelium accelerates triple-negative breast cancer with dependency on eEF2K

EMBO Mol Med. 2014 Dec;6(12):1542-60. doi: 10.15252/emmm.201404402.

Abstract

The tumor suppressors Pten and p53 are frequently lost in breast cancer, yet the consequences of their combined inactivation are poorly understood. Here, we show that mammary-specific deletion of Pten via WAP-Cre, which targets alveolar progenitors, induced tumors with shortened latency compared to those induced by MMTV-Cre, which targets basal/luminal progenitors. Combined Pten-p53 mutations accelerated formation of claudin-low, triple-negative-like breast cancer (TNBC) that exhibited hyper-activated AKT signaling and more mesenchymal features relative to Pten or p53 single-mutant tumors. Twenty-four genes that were significantly and differentially expressed between WAP-Cre:Pten/p53 and MMTV-Cre:Pten/p53 tumors predicted poor survival for claudin-low patients. Kinome screens identified eukaryotic elongation factor-2 kinase (eEF2K) inhibitors as more potent than PI3K/AKT/mTOR inhibitors on both mouse and human Pten/p53-deficient TNBC cells. Sensitivity to eEF2K inhibition correlated with AKT pathway activity. eEF2K monotherapy suppressed growth of Pten/p53-deficient TNBC xenografts in vivo and cooperated with doxorubicin to efficiently kill tumor cells in vitro. Our results identify a prognostic signature for claudin-low patients and provide a rationale for using eEF2K inhibitors for treatment of TNBC with elevated AKT signaling.

Keywords: Pten; eEF2K; p53; prognosis; triple‐negative breast cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Elongation Factor 2 Kinase / antagonists & inhibitors
  • Elongation Factor 2 Kinase / genetics
  • Elongation Factor 2 Kinase / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Epithelium / enzymology
  • Epithelium / metabolism
  • Female
  • Gene Deletion*
  • Humans
  • Mammary Glands, Human / enzymology
  • Mammary Glands, Human / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Oncogene Protein v-akt / genetics
  • Oncogene Protein v-akt / metabolism
  • PTEN Phosphohydrolase / genetics*
  • PTEN Phosphohydrolase / metabolism
  • Triple Negative Breast Neoplasms / drug therapy
  • Triple Negative Breast Neoplasms / enzymology*
  • Triple Negative Breast Neoplasms / genetics
  • Tumor Suppressor Protein p53 / genetics*
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • Enzyme Inhibitors
  • Tumor Suppressor Protein p53
  • Oncogene Protein v-akt
  • Elongation Factor 2 Kinase
  • PTEN Phosphohydrolase