Chapter 17 - Inhibitors targeting epigenetic modifications in cancer

Abstract

Epigenetics is an extraordinary mechanism by which our body controls genomic destiny without altering the underlying nucleotide sequence. Various epigenetic modifiers such as writers, readers, and erasers are involved in regulation of gene expression. However, any aberrancy in epigenetic regulation by these elements can lead to various abnormalities such as cancer and genetic diseases. Various epigenetic modifications such as DNA methylation, histone methylation, and acetylation have been observed in many cancers. Fragile X syndrome, Angelman's syndrome, and Prader Willi syndrome are some common genetic diseases caused by abnormal epigenetic regulation. Therefore, understanding epigenetic regulatory mechanisms in different diseases can lead to the development of various biomarkers having diagnostic potential or identifying potential drug targets. Epigenetic biomarkers also allow the detection of malignancies by noninvasive procedures using body fluids. Because epigenetic modifications are reversible, they can be effectively targeted for the treatment of various malignancies. Inhibiting abnormally expressed epigenetic regulators by various inhibitors has been shown to have the apoptotic effect, antitumor property, and regression in cancer states. Various preclinical and clinical trials have been performed in evaluating the efficacy of these inhibitors, and some of them have got FDA approval. In this chapter, we have summarized the epigenetic mechanics involved in cancer etiology. We also explored the diagnostic therapeutic advancements for targeting epigenetic regulatory mechanisms in cancer.