Inhibition of Histone Deacetylation Potentiates the Evolution of Acquired Temozolomide Resistance Linked to MGMT Upregulation in Glioblastoma Xenografts

Jun 8, 2012Clinical cancer research : an official journal of the American Association for Cancer Research

Blocking histone deacetylation may increase the development of drug resistance linked to MGMT in glioblastoma models

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Abstract

Upregulation of O6-methylguanine-DNA methyltransferase (MGMT) expression was observed in 3 of the 5 resistant glioblastoma multiforme xenografts.

  • Temozolomide resistance in glioblastoma multiforme may be linked to increased MGMT expression.
  • No significant changes in MGMT promoter methylation were found between parental and resistant tumor samples.
  • An association was detected between MGMT upregulation and higher levels of acetylation of a specific histone mark (H3K9-ac) along with lower levels of another mark (H3K9-me2) in certain resistant tumors.
  • In one resistant line, increased MGMT expression correlated with greater recruitment of specific transcription factors to the MGMT promoter.
  • Combined treatment with temozolomide and an HDAC inhibitor may enhance MGMT overexpression, contributing to the development of resistance.

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