Squelching glioblastoma stem cells by targeting REST for proteasomal degradation

Trends Neurosci. 2009 Nov;32(11):559-65. doi: 10.1016/j.tins.2009.07.005. Epub 2009 Sep 11.

Abstract

Glioblastoma brain tumors harbor a small population of cancer stem cells that are resistant to conventional chemotherapeutic and radiation treatments, and are believed responsible for tumor recurrence and mortality. The identification of the epigenetic molecular mechanisms that control self-renewal of glioblastoma stem cells will foster development of targeted therapeutic approaches. The transcriptional repressor REST, best known for its role in controlling cell fate decisions in neural progenitor cells, may also be crucial for cancer stem cell self-renewal. Two novel mechanisms for regulating the stability of REST have recently been revealed: these involve the telomere-binding protein TRF2 and the ubiquitin E3 ligase SCFbeta-TrCP. Reduced TRF2 binding to REST, and increased SCFbeta-TrCP activity, target REST for proteasomal degradation and thereby inhibit cancer stem cell proliferation. Neurological side effects of treatments that target REST and TRF2 may be less severe than conventional brain tumor treatments because postmitotic neurons do not express REST and have relatively stable telomeres.

Publication types

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

MeSH terms

  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / metabolism*
  • Brain Neoplasms / pathology
  • Cell Proliferation / drug effects
  • Drug Design
  • Glioblastoma / drug therapy
  • Glioblastoma / metabolism*
  • Glioblastoma / pathology
  • Humans
  • Neoplastic Stem Cells / drug effects
  • Neoplastic Stem Cells / metabolism*
  • Neoplastic Stem Cells / pathology
  • Repressor Proteins / drug effects
  • Repressor Proteins / metabolism*
  • SKP Cullin F-Box Protein Ligases / metabolism*
  • Telomeric Repeat Binding Protein 2 / metabolism
  • Tumor Cells, Cultured

Substances

  • RE1-silencing transcription factor
  • Repressor Proteins
  • Telomeric Repeat Binding Protein 2
  • SKP Cullin F-Box Protein Ligases