The Development of Epigenetics and Related Inhibitors for Targeted Drug Design in Cancer Therapy

Author(s): Na Liu, Rongtong Zhao, Yue Ma, Dongyuan Wang, Chen Yan, Dongxian Zhou*, Feng Yin*, Zigang Li*

Journal Name: Current Topics in Medicinal Chemistry

Volume 18 , Issue 28 , 2018

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Graphical Abstract:


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.

Keywords: Epigenetic targets, Inhibitors, Cancer therapy, Drug discovery, DNMT, HDAC.

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Article Details

Year: 2018
Published on: 14 November, 2018
Page: [2380 - 2394]
Pages: 15
DOI: 10.2174/1568026618666181115092623
Price: $65

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