Epigenetics is defined as the stable and heritable alternations in gene expression without
changing the DNA nucleotide sequence. The initiation and progression of cancer result from not only
genetic mutation, but also aberrant epigenetic regulation, such as DNA methylation and histones acetylation.
Although Genetic alternations cannot be reversed, epigenetic modification is a dynamic and reversible
process. Over the past few decades, much progress has been made in the research of epigenetic
medications and a variety of drugs have been developed targeting at epigenetic regulatory proteins,
which are capable of restoring malignant cancer cells to the normal state. The epigenetic drugs currently
approved for cancer treatment mainly target at DNA methylation and histones acetylation. In addition,
there are a great many epigenetic drugs in clinical trials for cancer therapy, such as inhibitors of DNA
methyltransferases, histone deacetylases, histone methyltransferases, lysine specific demethylases, and
BET (bromodomain and extra-terminal domain) family proteins. We will discuss the latest developments
of these inhibitors and their applications in cancer therapy.