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Cancer is a major global public health problem. According to the latest global cancer data released by the World Health Organization (WHO), in 2021, the cancer burden will rise to 19.3 million new cases and 10.0 million cancer deaths 2020. Epigenetics refers to the heritable change of gene function without ...

Cancer is a major global public health problem. According to the latest global cancer data released by the World Health Organization (WHO), in 2021, the cancer burden will rise to 19.3 million new cases and 10.0 million cancer deaths 2020. Epigenetics refers to the heritable change of gene function without the change of gene DNA sequence, which eventually leads to the change of phenotype. Extensive studies have shown that epigenetic dysregulation contributes to cancer initiation, maintenance, and evolution. By 2021, 9 epigenetic agents have been approved by the U.S. FDA for cancer treatment.

However, some challenges still need to be overcome for this field to progress. Currently, epigenetic drugs can not be widely used to treat various cancers. Moreover, the efficacy is not ideal, and many drugs have low bioavailability, poor stability, high toxicity, etc. Therefore, combinations of immunotherapies and epigenetic therapies will be the next frontier.

The Research Topic is the development of new epigenetic agents and combinations of immunotherapies and epigenetic therapies. Under this Research Topic, we welcome high-quality original research articles, letters, and reviews. The following directions are especially welcome but are not limited to:

• DNA methyltransferase (DNMT) modulators.
• Histone deacetylase (HDAC) modulators.
• Sirtuins modulators.
• Isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) modulators.
• EZH2 methyltransferase modulators.
• Bromodomain and extra terminal (BET) modulators.
• Lysine-specific demethylase 1 (LSD1) modulators.
• Combinations of epigenetic agents and other anticancer therapies such as immunotherapies.

Keywords: Epigenetic, Anticancer, Inhibitor, Design, Synthesis, Structure-activity relationship studies


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