Combination Epigenetic Therapy

Epigenetic alterations cause changes in DNA and histone modifications, microRNAs expression and in this way cause variances in genes expression and cell phenotype. The most common abnormal epigenetic changes resulting multiple diseases increase with age. As a result, gene expression changes cause a variety of diseases, including cancer. The essential aim in developing novel epigenetic therapeutics is to understand the molecular mechanisms of abnormal DNA and posttranslational histone modifications implicated in tumor suppressors gene silencing or activation of oncogenes. The use of drugs inducing epigenetic changes, such as inhibitors of histone methyltransferases (HMTs), histone deacetylases (HDACs), DNA methyltransferases (DNMTs) and others, and ongoing epigenetic studies helps in explaining some forms of cancer-specific attributes. These compounds can be applied alone or in combinations in the treatment of various diseases, including cancer. Recently, other potential inhibitors and modifiers that regulate mitochondrial activity have been of particular interest. They will be briefly reviewed and the combined use of epigenetic-modifying drugs will be analyzed.