IGF1R Is a Potential New Therapeutic Target for HGNET-BCOR Brain Tumor Patients

Int J Mol Sci. 2019 Jun 21;20(12):3027. doi: 10.3390/ijms20123027.

Abstract

(1) Background: The high-grade neuroepithelial tumor of the central nervous system with BCOR alteration (HGNET-BCOR) is a highly malignant tumor. Preclinical models and molecular targets are urgently required for this cancer. Previous data suggest a potential role of insulin-like growth factor (IGF) signaling in HGNET-BCOR. (2) Methods: The primary HGNET-BCOR cells PhKh1 were characterized by western blot, copy number variation, and methylation analysis and by electron microscopy. The expression of IGF2 and IGF1R was assessed by qRT-PCR. The effect of chemotherapeutics and IGF1R inhibitors on PhKh1 proliferation was tested. The phosphorylation of IGF1R and downstream molecules was assessed by western blot. (3) Results: Phkh1 cells showed a DNA methylation profile compatible with the DNA methylation class "HGNET-BCOR" and morphologic features of cellular cannibalism. IGF2 and IGF1R were highly expressed by three HGNET-BCOR tumor samples and PhKh1 cells. PhKh1 cells were particularly sensitive to vincristine, vinblastine, actinomycin D (IC50 < 10 nM for all drugs), and ceritinib (IC50 = 310 nM). Ceritinib was able to abrogate the proliferation of PhKh1 cells and blocked the phosphorylation of IGF1R and AKT. (4) Conclusion: IGF1R is as an attractive target for the development of new therapy protocols for HGNET-BCOR patients, which may include ceritinib and vinblastine.

Keywords: HGNET-BCOR; IGF1R; IGF2; ceritinib; vinblastine.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / genetics
  • Brain Neoplasms / metabolism
  • DNA Methylation / drug effects
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Insulin-Like Growth Factor II / genetics
  • Insulin-Like Growth Factor II / metabolism
  • Male
  • Molecular Targeted Therapy
  • Neoplasms, Neuroepithelial / drug therapy*
  • Neoplasms, Neuroepithelial / genetics
  • Neoplasms, Neuroepithelial / metabolism
  • Proto-Oncogene Proteins / genetics
  • Pyrimidines / pharmacology*
  • Receptor, IGF Type 1
  • Receptors, Somatomedin / genetics
  • Receptors, Somatomedin / metabolism*
  • Repressor Proteins / genetics
  • Sulfones / pharmacology*
  • Tumor Cells, Cultured
  • Vinblastine / pharmacology*

Substances

  • Antineoplastic Agents
  • BCOR protein, human
  • IGF1R protein, human
  • IGF2 protein, human
  • Proto-Oncogene Proteins
  • Pyrimidines
  • Receptors, Somatomedin
  • Repressor Proteins
  • Sulfones
  • Vinblastine
  • Insulin-Like Growth Factor II
  • Receptor, IGF Type 1
  • ceritinib