Present Status Of Epigenetic Drugs In Cancer Treatment

Epigenetic changes such as promoter specific DNA hypermethylation and histone deacetylation cause tumor suppressor genes to become transcriptionally silent and contribute to malignant transformation. DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors can reactivate silenced genes, block cell cycle and induce cell apoptosis which provides rationale for their use in cancer treatment. DNMT and HDAC inhibitors have therefore emerged as an effective strategy against cancer. Epigenetic modifications have a key role in the pathophysiology of many cancers such as myelodysplastic syndrome (MDS), lymphoma, and leukemia and the use of drugs targeting epigenetic changes has become a topic of intense interest in cancer research. The role of transcriptional repression through epigenetic modulation in carcinogenesis has clinically validated the use of inhibitors of DNMT and HDAC. Epigenetic changes can be pharmacologically reversed resulting in gene re-expression.