ERG deregulation induces IGF-1R expression in prostate cancer cells and affects sensitivity to anti-IGF-1R agents

Oncotarget. 2015 Jun 30;6(18):16611-22. doi: 10.18632/oncotarget.3425.

Abstract

Identifying patients who may benefit from targeted therapy is an urgent clinical issue in prostate cancer (PCa). We investigated the molecular relationship between TMPRSS2-ERG (T2E) fusion gene and insulin-like growth factor receptor (IGF-1R) to optimize the use of IGF-1R inhibitors.IGF-1R was analyzed in cell lines and in radical prostatectomy specimens in relation to T2E status. ERG binding to IGF-1R promoter was evaluated by chromatin immunoprecipitation (ChIP). Sensitivity to anti-IGF-1R agents was evaluated alone or in combination with anti-androgen abiraterone acetate in vitro at basal levels or upon ERG modulation.IGF-1R analysis performed in PCa cells or clinical samples showed that T2E expression correlated with higher IGF-1R expression at mRNA and protein levels. Genetic modulation of ERG directly affected IGF-1R protein levels in vitro. ChIP analysis showed that ERG binds IGF-1R promoter and that promoter occupancy is higher in T2E-positive cells. IGF-1R inhibition was more effective in cell lines expressing the fusion gene and combination of IGF-1R inhibitors with abiraterone acetate produced synergistic effects in T2E-expressing cells.Here, we provide the rationale for use of T2E fusion gene to select PCa patients for anti-IGF-1R treatments. The combination of anti-IGF-1R-HAbs with an anti-androgen therapy is strongly advocated for patients expressing T2E.

Keywords: ETS fusion genes; anti-IGF-1R agents; insulin-like growth factor receptor 1; prostate cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abiraterone Acetate / pharmacology
  • Androgen Antagonists / pharmacology*
  • Antineoplastic Agents / pharmacology
  • Biomarkers, Tumor / genetics
  • Cell Line, Tumor
  • DNA-Binding Proteins / metabolism
  • Humans
  • Male
  • Promoter Regions, Genetic / genetics
  • Prostate / pathology
  • Prostate / surgery
  • Prostatic Neoplasms / pathology*
  • Protein Binding
  • Receptor, IGF Type 1 / antagonists & inhibitors*
  • Receptor, IGF Type 1 / biosynthesis
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Serine Endopeptidases / genetics*
  • Serine Endopeptidases / metabolism
  • Trans-Activators / genetics*
  • Trans-Activators / metabolism
  • Transcriptional Regulator ERG

Substances

  • Androgen Antagonists
  • Antineoplastic Agents
  • Biomarkers, Tumor
  • DNA-Binding Proteins
  • ERG protein, human
  • Recombinant Fusion Proteins
  • Trans-Activators
  • Transcriptional Regulator ERG
  • Receptor, IGF Type 1
  • Serine Endopeptidases
  • TMPRSS2 protein, human
  • Abiraterone Acetate