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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Current Status of Epigenetics and Anticancer Drug Discovery

Author(s): Ping Jin and Xiaofei Chen

Volume 16 , Issue 6 , 2016

Page: [699 - 712] Pages: 14

DOI: 10.2174/1871520616666151116124432

Price: $65


In recent years, there has been an expansion of the understanding of how epigenetic dysregulation plays a role in tumorigenesis, progression, metastasis and treatment resistance. Evidence has focused on two common and well-studied “epigenetic codes”, i.e., DNA methylation and histone posttranslational modification, which regulate the transcriptional status in various types of cancer and the corresponding target agents.

Aside from “writers” and “erasers”, which refer to enzymes that catalyze and remove posttranslational modifications, respectively, “readers” bind to target proteins and recruit “writers” and “erasers” for regulating gene expression. A number of selective and potent anticancer compounds have been reported, some of which are in preclinical or clinical trials that have shown promising results, primarily against malignant neoplasms such as hematologic malignancies, with the subsequent emerging development of both monotherapy and co-administration with traditional cytotoxic medicines against solid tumors. Second-generation epigenetic agents such as EZH2 and BET inhibitors have greatly progressed. Epigenetic dysregulation has also provided feasibility for the diagnosis and treatment of cancer. In this review, we summarize the progress in epigenetics and drug discovery for cancer and certain clinical trials that may provide a perspective for future development.

Keywords: Epigenetic, anticancer drug discovery, DNA methylation, histone posttranslational modification.

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