Targeting NF-κB in glioblastoma: A therapeutic approach

Sci Adv. 2016 Jan 8;2(1):e1501292. doi: 10.1126/sciadv.1501292. eCollection 2016 Jan.

Abstract

Glioblastoma multiforme (GBM) is the most common and lethal form of intracranial tumor. We have established a lentivirus-induced mouse model of malignant gliomas, which faithfully captures the pathophysiology and molecular signature of mesenchymal human GBM. RNA-Seq analysis of these tumors revealed high nuclear factor κB (NF-κB) activation showing enrichment of known NF-κB target genes. Inhibition of NF-κB by either depletion of IκB kinase 2 (IKK2), expression of a IκBαM super repressor, or using a NEMO (NF-κB essential modifier)-binding domain (NBD) peptide in tumor-derived cell lines attenuated tumor proliferation and prolonged mouse survival. Timp1, one of the NF-κB target genes significantly up-regulated in GBM, was identified to play a role in tumor proliferation and growth. Inhibition of NF-κB activity or silencing of Timp1 resulted in slower tumor growth in both mouse and human GBM models. Our results suggest that inhibition of NF-κB activity or targeting of inducible NF-κB genes is an attractive therapeutic approach for GBM.

Keywords: Gliomas; NF-κB inhibitors; TIMP1; Xenografts.

Publication types

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

MeSH terms

  • Animals
  • Brain Neoplasms / genetics*
  • Cell Line, Tumor
  • Gene Expression Regulation, Neoplastic / genetics
  • Glioblastoma / genetics*
  • Humans
  • I-kappa B Kinase / genetics
  • Mice
  • Mice, Inbred NOD
  • Mice, SCID
  • NF-kappa B / genetics*
  • Peptides / genetics
  • Signal Transduction / genetics
  • Up-Regulation / genetics

Substances

  • NF-kappa B
  • Peptides
  • I-kappa B Kinase