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Epigenetic mechanisms are essential for the development of multicellular organisms. Unfortunately, these mechanisms can become misregulated to cause the inappropriate expression of genes resulting in diseases such as cancer. It has been amply documented that epigenetics cooperates with genetics to cause human cancer and profound changes in the epigenome are observed in human cancer cells. Our interests are in understanding the nature of these changes and to design drugs which can reverse them, thus restoring normal pathways to cancer cells. We are now entering the era of epigenetic therapy and this approach has become a clinical reality.