, Volume 71, Issue 18, pp 2391–2403

Epigenetic-Based Therapies in Cancer

Progress to Date
Leading Article

DOI: 10.2165/11596690-000000000-00000

Cite this article as:
Song, SH., Han, SW. & Bang, YJ. Drugs (2011) 71: 2391. doi:10.2165/11596690-000000000-00000


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.

Copyright information

© Adis Data Information BV 2011

Authors and Affiliations

  1. 1.Cancer Research InstituteSeoul National University College of MedicineSeoulSouth Korea
  2. 2.Division of Hematology/Medical Oncology, Department of Internal MedicineSeoul National University College of MedicineJongno-gu, SeoulSouth Korea

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