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.
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