Identification of a novel synthetic lethal vulnerability in non-small cell lung cancer by co-targeting TMPRSS4 and DDR1

Sci Rep. 2019 Oct 28;9(1):15400. doi: 10.1038/s41598-019-51066-3.

Abstract

Finding novel targets in non-small cell lung cancer (NSCLC) is highly needed and identification of synthetic lethality between two genes is a new approach to target NSCLC. We previously found that TMPRSS4 promotes NSCLC growth and constitutes a prognostic biomarker. Here, through large-scale analyses across 5 public databases we identified consistent co-expression between TMPRSS4 and DDR1. Similar to TMPRSS4, DDR1 promoter was hypomethylated in NSCLC in 3 independent cohorts and hypomethylation was an independent prognostic factor of disease-free survival. Treatment with 5-azacitidine increased DDR1 levels in cell lines, suggesting an epigenetic regulation. Cells lacking TMPRSS4 were highly sensitive to the cytotoxic effect of the DDR1 inhibitor dasatinib. TMPRSS4/DDR1 double knock-down (KD) cells, but not single KD cells suffered a G0/G1 cell cycle arrest with loss of E2F1 and cyclins A and B, increased p21 levels and a larger number of cells in apoptosis. Moreover, double KD cells were highly sensitized to cisplatin, which caused massive apoptosis (~40%). In vivo studies demonstrated tumor regression in double KD-injected mice. In conclusion, we have identified a novel vulnerability in NSCLC resulting from a synthetic lethal interaction between DDR1 and TMPRSS4.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / genetics*
  • Adenocarcinoma / pathology
  • Animals
  • Apoptosis / drug effects
  • Biomarkers, Tumor / genetics*
  • Cell Line, Tumor
  • Cisplatin / toxicity
  • DNA Methylation
  • Dasatinib / toxicity
  • Discoidin Domain Receptor 1 / genetics*
  • Drug Resistance, Neoplasm
  • Humans
  • Lung Neoplasms / genetics*
  • Lung Neoplasms / pathology
  • Membrane Proteins / genetics*
  • Mice
  • Promoter Regions, Genetic
  • Serine Endopeptidases / genetics*
  • Synthetic Lethal Mutations*

Substances

  • Biomarkers, Tumor
  • Membrane Proteins
  • DDR1 protein, human
  • Discoidin Domain Receptor 1
  • Serine Endopeptidases
  • TMPRSS4 protein, human
  • Cisplatin
  • Dasatinib