From Bench to Bedside: Targeting Epigenetics for Cancer Therapy

Gui-deng Li, Jin-xu Fang


The initiation and progression of cancer not only involves genetic abnormalities, but also epigenetic alterations, such as DNA methylation and histone modifications. Epigenetics refers to the heritable changes that do not involve any structural changes in the target gene, i.e., DNA sequence and protein sequence. Thus, these epigenetic aberrations are potentially reversible, allowing the malignant cells to revert to a state with more normal characteristics. The use of epigenetics is emerging as an effective and promising approach to treat cancer. Epigenetic drugs, which target two well-known epigenetic pathways, namely, DNA methyltransferases and histone deacetylases, are already being applied for the cancer treatment. In the current study, an overview regarding the understanding of epigenetic alterations in the development of cancer and the current state of epigenetic drug discovery is provided.



cancer epigenetics, DNA methylation, histone modifications, epigenetic drugs

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