論文

査読有り
2017年12月

HDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications

Leukemia
  • Takeshi Harada
  • ,
  • Ohguchi Hiroto
  • ,
  • Grondin Yohann
  • ,
  • Kikuchi Shohei
  • ,
  • Sagawa Morihiko
  • ,
  • Tai Yu-Tzu
  • ,
  • Mazitschek Ralph
  • ,
  • Hideshima Teru
  • ,
  • Anderson C. Kenneth

Vol.31
No.12
開始ページ
2670
終了ページ
2677
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1038/leu.2017.144

Epigenetic signaling pathways are implicated in tumorigenesis and therefore histone deacetylases (HDACs) represent novel therapeutic targets for cancers, including multiple myeloma (MM). Although non-selective HDAC inhibitors show anti-MM activities, unfavorable side effects limit their clinical efficacy. Isoform- and/or class-selective HDAC inhibition offers the possibility to maintain clinical activity while avoiding adverse events attendant to broad non-selective HDAC inhibition. We have previously reported that HDAC3 inhibition, either by genetic knockdown or selective inhibitor BG45, abrogates MM cell proliferation. Here we show that knockdown of HDAC3, but not HDAC1 or HDAC2, as well as BG45, downregulate expression of DNA methyltransferase 1 (DNMT1) mediating MM cell proliferation. DNMT1 expression is regulated by c-Myc, and HDAC3 inhibition triggers degradation of c-Myc protein. Moreover, HDAC3 inhibition results in hyperacetylation of DNMT1, thereby reducing the stability of DNMT1 protein. Combined inhibition of HDAC3 and DNMT1 with BG45 and DNMT1 inhibitor 5-azacytidine (AZA), respectively, triggers synergistic downregulation of DNMT1, growth inhibition and apoptosis in both MM cell lines and patient MM cells. Efficacy of this combination treatment is confirmed in a murine xenograft MM model. Our results therefore provide the rationale for combination treatment using HDAC3 inhibitor with DNMT1 inhibitor to improve patient outcome in MM.

リンク情報
DOI
https://doi.org/10.1038/leu.2017.144
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/28490812
ID情報
  • DOI : 10.1038/leu.2017.144
  • ISSN : 1476-5551
  • PubMed ID : 28490812

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