ID1 Is Critical for Tumorigenesis and Regulates Chemoresistance in Glioblastoma

Cancer Res. 2019 Aug 15;79(16):4057-4071. doi: 10.1158/0008-5472.CAN-18-1357. Epub 2019 Jul 10.

Abstract

Glioblastoma is the most common primary brain tumor in adults. While the introduction of temozolomide chemotherapy has increased long-term survivorship, treatment failure and rapid tumor recurrence remains universal. The transcriptional regulatory protein, inhibitor of DNA-binding-1 (ID1), is a key regulator of cell phenotype in cancer. We show that CRISPR-mediated knockout of ID1 in glioblastoma cells, breast adenocarcinoma cells, and melanoma cells dramatically reduced tumor progression in all three cancer systems through transcriptional downregulation of EGF, which resulted in decreased EGFR phosphorylation. Moreover, ID1-positive cells were enriched by chemotherapy and drove tumor recurrence in glioblastoma. Addition of the neuroleptic drug pimozide to inhibit ID1 expression enhanced the cytotoxic effects of temozolomide therapy on glioma cells and significantly prolonged time to tumor recurrence. Conclusively, these data suggest ID1 could be a promising therapeutic target in patients with glioblastoma. SIGNIFICANCE: These findings show that the transcriptional regulator ID1 is critical for glioblastoma initiation and chemoresistance and that inhibition of ID1 enhances the effect of temozolomide, delays tumor recurrence, and prolongs survival.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Alkylating / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / mortality
  • Brain Neoplasms / pathology
  • Breast Neoplasms / pathology
  • Drug Resistance, Neoplasm / drug effects
  • Drug Resistance, Neoplasm / physiology*
  • ErbB Receptors / metabolism
  • Female
  • Gene Expression Regulation, Neoplastic
  • Glioblastoma / drug therapy*
  • Glioblastoma / mortality
  • Glioblastoma / pathology
  • Humans
  • Inhibitor of Differentiation Protein 1 / antagonists & inhibitors
  • Inhibitor of Differentiation Protein 1 / genetics
  • Inhibitor of Differentiation Protein 1 / metabolism*
  • Melanoma / pathology
  • Mice, Inbred NOD
  • Phosphorylation
  • Pimozide / administration & dosage
  • Pimozide / pharmacology
  • Temozolomide / administration & dosage
  • Temozolomide / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents, Alkylating
  • ID1 protein, human
  • Inhibitor of Differentiation Protein 1
  • Pimozide
  • EGFR protein, human
  • ErbB Receptors
  • Temozolomide

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