MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer

Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. doi: 10.1073/pnas.1814742116. Epub 2019 Feb 4.

Abstract

Chemoresistance is a severe outcome among patients with ovarian cancer that leads to a poor prognosis. MCL1 is an antiapoptotic member of the BCL-2 family that has been found to play an essential role in advancing chemoresistance and could be a promising target for the treatment of ovarian cancer. Here, we found that deubiquitinating enzyme 3 (DUB3) interacts with and deubiquitinates MCL1 in the cytoplasm of ovarian cancer cells, which protects MCL1 from degradation. Furthermore, we identified that O6-methylguanine-DNA methyltransferase (MGMT) is a key activator of DUB3 transcription, and that the MGMT inhibitor PaTrin-2 effectively suppresses ovarian cancer cells with elevated MGMT-DUB3-MCL1 expression both in vitro and in vivo. Most interestingly, we found that histone deacetylase inhibitors (HDACis) could significantly activate MGMT/DUB3 expression; the combined administration of HDACis and PaTrin-2 led to the ideal therapeutic effect. Altogether, our results revealed the essential role of the MGMT-DUB3-MCL1 axis in the chemoresistance of ovarian cancer and identified that a combined treatment with HDACis and PaTrin-2 is an effective method for overcoming chemoresistance in ovarian cancer.

Keywords: DUB3; MCL1; MGMT; chemoresistance; ovarian cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • DNA Modification Methylases / genetics*
  • DNA Repair Enzymes / genetics*
  • Drug Resistance, Neoplasm / genetics
  • Endopeptidases / genetics*
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Histone Deacetylase Inhibitors / pharmacology
  • Humans
  • Myeloid Cell Leukemia Sequence 1 Protein / genetics*
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / genetics
  • Ovarian Neoplasms / pathology
  • Signal Transduction / drug effects
  • Tumor Suppressor Proteins / genetics*

Substances

  • Histone Deacetylase Inhibitors
  • MCL1 protein, human
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Tumor Suppressor Proteins
  • DNA Modification Methylases
  • MGMT protein, human
  • Endopeptidases
  • USP17L2 protein, human
  • DNA Repair Enzymes