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About Epigenetics
The term epigenetic regulation is commonly used for post-translational covalent modifications of histones and other chromatin-remodeling complexes, which determines whether a gene is accessible and hence, expressed or repressed.
Covalent modifications involved in epigenetic regulation include DNA methylation, histone acetylation, and histone methylation. These modifications and the removal of these are catalyzed by specific enzymes, which often are found mis-expressed in various human diseases, including cancer. Thus, the enzymes becomes extremely important, since they regulate genes that are required for differentiation and maintenance of cells in specific states, and the deregulation of the enzymes can therefore lead to the development of cancer.
The development of so-called epigenetic drugs is now regarded as an important point of intervention for the treatment of cancer. In fact, the first drugs targeting histone deacetylases (HDAC inhibitors) and DNA methyltransferases (DNMT inhibitors) have recently been approved for the treatment of cutaneous T cell lymphoma and myeolodysplastic syndrome, respectively. Moreover, several other compounds are in the pipeline that inhibits targets histone deacetylation, histone methyltransferases (HMT inhibitors) or DNA methyltranferases (DNMT inhibitors).
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