Epigenetics process is the heritable change in gene function that does not involve changes in
the DNA sequence. Until now, several types of epigenetic mechanisms have been characterized, including
DNA methylation, histone modification (acetylation, methylation, etc.), nucleosome remodeling, and
noncoding RNAs. With the biological investigations of these modifiers, some of them are identified as
promoters in the process of various diseases, such as cancer, cardiovascular disease and virus infection.
Epigenetic changes may serve as potential “first hits” for tumorigenesis. Hence, targeting epigenetic
modifiers is being considered as a promising way for disease treatment. To date, six agents in two epigenetic
target classes (DNMT and HDAC) have been approved by the US Food and Drug Administration
(FDA). Most of these drugs are applied in leukemia, lymphoma therapy, or are combined with other
drugs for the treatment of solid tumor. Due to the rapid development of epigenetics and epigenetics targeted
drugs, it is becoming an emerging area in targeted drug design.
