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The aberrantly modified epigenome confers unique features on tumor cells, including sustained proliferative potential, resistance to growth-suppressive or cell death signals, augmented replicative immortality, invasion, and metastasis. As a result, epigenetic abnormalities exhibit significant impacts on all stages of oncogenesis from its onset to progression to metastasis. DNA cytosine methylation–demethylation is frequently disrupted, and its reversibility makes DNA methylation dynamics an attractive therapeutic target.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":40,"@type":76,"position":81},"https://docshare.wps.com/document/research-report/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/epigenetic-regulators-of-dna-cytosine-modification-promising-targets-for-cancer-therapy/377690/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/epigenetic-regulators-of-dna-cytosine-modification-promising-targets-for-cancer-therapy/377690.png","ImageObject",300,407,{"name":92,"@type":93},"Patrick","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-09-26","2026-09-24",true,{"@type":102,"interactionType":103,"userInteractionCount":81},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"Why are epigenetic modifications important in cancer?","Question",{"text":112,"@type":113},"They regulate gene expression and their dysregulation is commonly observed in cancers. 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Epigenetic Regulators of DNA Cytosine Modification: Promising Targets for Cancer Therapy. Biomedicines 2023, 11, 654 . [https://doi.org/10.3390/](https://doi.org/10.3390/)[ ](https://doi.org/10.3390/)biomedicines11030654  \nAcademic Editor: Chiara Brignole  \nReceived: 30 January 2023  \nRevised: 16 February 2023  \nAccepted: 20 February 2023  \nPublished: 21 February 2023  \nCopyright: © 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ([https://](https://)[ ](https://)[creativecommons.org/licenses/by/](creativecommons.org/licenses/by/)[ ](creativecommons.org/licenses/by/)[4.0/](4.0/)) .  \n1 Department of Biological Sciences, Ulsan National Institute of Science and Technology, Ulsan 44919, Republic of Korea  \n2 Department of Life Sciences, Jeonbuk National University, Jeonju 54896, Republic of Korea  \n3 Center for Genomic Integrity, Institute for Basic Science, Ulsan 44919, Republic of Korea  \n* [Correspondence: jan@jbnu.ac.kr](Correspondence: jan@jbnu.ac.kr) (J.A.); [mgko@unist.ac.kr](mgko@unist.ac.kr) (M.K.); Tel.: +82-63-270-3365 (J.A.); +82-52-217-2516 (M.K.)  \nAbstract: Epigenetic modifications are crucial regulators of gene expression that critically impact cell lineage differentiation, survival, and proliferation, and dysregulations are commonly observed in various cancers. The aberrantly modified epigenome confers unique features on tumor cells, including sustained proliferative potential, resistance to growth-suppressive or cell death signals, augmented replicative immortality, invasion, and metastasis. As a result, epigenetic abnormalities exhibit significant impacts on all stages of oncogenesis from its onset to progression to metastasis. Among various epigenetic mechanisms in mammals, DNA cytosine methylation–demethylationis recurrently disrupted in cancers. Due to its inherent reversibility, targeting DNA methylation dynamics has gained tremendous attention as a promising therapeutic option that can ameliorate the effects of cancer-specific epigenetic abnormalities by restoring normal conditions. Various small molecules targeting DNA (de)methylation regulators have been developed as potential cancer therapeutics, some of which are approved for usage in clinics. Clinical trials of many other molecules are underway for both hematological malignancies and solid tumors. In this review, we discuss the DNA methylation/demethylation pathway as a promising target for therapeutic intervention in cancer and highlight the development of various epigenetic drugs targeting DNA-modifying enzymes such as DNA methyltransferases (DNMTs) and ten-eleven translocation (TET) enzymes.  \nKeywords: epigenetics; DNMT; TET dioxygenases; DNA methylation and demethylation; small molecules; cancer therapy  \n1. Introduction  \nIn eukaryotes, genomic DNA is condensed into chromatin by wrapping around histone octamers in the nucleus. Euchromatin has an open structure and encompasses the majority of transcriptionally active genes. Conversely, a highly condensed chromatin structure termed heterochromatin usually contains silent genes and is important for guarding genomic integrity by protecting the genome from transposon activation and exerting key regulatory functions. Epigenetics is defined by a heritable genomic mechanism that reversibly influences gene expression without changes in DNA sequences [1,2] . Chromatin structure and accessibility to transcription factors are dynamically regulated by epigenetic mechanisms such as histone modification, DNA methylation, and nucleosome mobilization.  \nThe two best-studied epigenetic modifications are DNA and histone modifications [1,2], which are catalyzed by “writers”, includi","cbCaihMdD9yfgDii","https://ap.wps.com/l/cbCaihMdD9yfgDii","pdf",13306473,22,"English","# Introduction\n## Epigenetic regulation and chromatin context\n## Writers, readers, and erasers of epigenetic marks","[{\"question\":\"Why are epigenetic modifications important in cancer?\",\"answer\":\"They regulate gene expression and their dysregulation is commonly observed in cancers. Aberrant epigenetic states support tumor growth, survival, invasion, and metastasis across oncogenesis stages.\"},{\"question\":\"What role does DNA cytosine methylation–demethylation play as a therapeutic target?\",\"answer\":\"DNA methylation/demethylation is recurrently disrupted in cancers. Because this process is inherently reversible, targeting it can help restore more normal conditions and counter cancer-specific epigenetic abnormalities.\"},{\"question\":\"Which enzymes and mechanisms are highlighted in the review?\",\"answer\":\"The review focuses on DNA methylation/demethylation pathways and therapeutic development targeting DNA-modifying enzymes, especially DNA methyltransferases (DNMTs) and TET enzymes, along with related epigenetic regulatory concepts.\"}]","Epigenetic Regulators of DNA Cytosine Modification: Promising Targets for Cancer Therapy | PDF",1790226687,55]