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Epigenetic-Based Therapies in Cancer

Progress to Date

Drugs volume 71, pages 2391–2403 (2011)Cite this article

Abstract

Epigenetic gene silencing is a hallmark of cancer cells. Two important types of epigenetic changes are DNA methylation and histone modification. These modifications are catalysed by DNA methyltransferases (DNMTs) and histone deacetylases (HDACs), resulting in chromatin structure changes and gene inactivation. Interestingly, inhibition of these enzymes is known to induce differentiation or apoptosis of cancer cells. Therefore, DNMTs and HDACs have become attractive therapeutic targets. In recent years, many different DNMT and HDAC inhibitors have been developed, and multiple molecular mechanisms through which these agents exert anti-cancer effects have been identified. While a large number of clinical trials are ongoing, hypomethylating agents and HDAC inhibitors seem to be promising for treating several types of cancer. Moreover, developing effective strategies of combining epigenetic therapy with conventional chemotherapy will be one of the major challenges in the future.

We briefly review current advances in epigenetic therapies with a focus on recently reported clinical trials.

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Acknowledgements

This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (2011-0021123) and by a research grant from the Cancer Research Institute, Seoul National University (2009, 2010). Dr Yung-Jue Bang has received honoraria for consultancies from Merck and Novartis, and received research grants from Merck. Drs Sang-Hyun Song and Sae-Won Han have no conflicts of interest that are directly relevant to the content of this article.

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  1. Cancer Research Institute, Seoul National University College of Medicine, Seoul, South Korea

    Sang-Hyun Song, Sae-Won Han &  Yung-Jue Bang MD, PhD

  2. Division of Hematology/Medical Oncology, Department of Internal Medicine, Seoul National University College of Medicine, 101 Daehang-ro, Jongno-gu, Seoul, 110-744, South Korea

    Sae-Won Han &  Yung-Jue Bang MD, PhD

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  1. Sang-Hyun Song
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Song, SH., Han, SW. & Bang, YJ. Epigenetic-Based Therapies in Cancer. Drugs 71, 2391–2403 (2011). https://doi.org/10.2165/11596690-000000000-00000

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Keywords

  • HDAC Inhibitor
  • Acute Myeloid Leukaemia
  • Nucleoside Analogue
  • Vorinostat
  • Decitabine