[{"data":1,"prerenderedAt":-1},["ShallowReactive",2],{"doc-seo-373036-105":3,"detail-sidebar-cat-0-en-105":81,"doc-detail-373036-en":131},{"code":4,"msg":5,"data":6},0,"ok",{"site_id":7,"language":8,"slug":9,"title":10,"keywords":11,"description":12,"schema_data":13,"social_meta":74,"head_meta":76,"extra_data":78,"updated_unix":80},105,"en","epigenetic-drugs-in-cancer-therapy","Epigenetic drugs in cancer therapy","","Genetic and epigenetic alterations of DNA drive cancer initiation and progression. Epigenetic changes remodel chromatin structure and DNA accessibility, thereby influencing replication, repair, and transcription; they are reversible and include DNA methylation, histone acetylation, and histone methylation. These dysregulated mechanisms become therapeutic targets. Epigenetic drugs (epi-drugs) such as DNMT, HDAC, HMT, and BET inhibitors have achieved clinical success, and combinations with standard chemotherapy show promising anti-cancer effects in pre-clinical and clinical studies, alongside discussion of side effects, limitations, delivery approaches, and tumor epigenetic biomarkers.",{"@graph":14,"@context":73},[15,34,56],{"@type":16,"itemListElement":17},"BreadcrumbList",[18,23,27,31],{"item":19,"name":20,"@type":21,"position":22},"https://docshare.wps.com","Home","ListItem",1,{"item":24,"name":25,"@type":21,"position":26},"https://docshare.wps.com/document/","Document",2,{"item":28,"name":29,"@type":21,"position":30},"https://docshare.wps.com/document/healthcare/","Healthcare",3,{"item":32,"name":10,"@type":21,"position":33},"https://docshare.wps.com/document/epigenetic-drugs-in-cancer-therapy/373036/",4,{"url":32,"name":10,"@type":35,"image":36,"author":41,"headline":10,"publisher":44,"fileFormat":47,"inLanguage":8,"description":12,"dateModified":48,"datePublished":49,"encodingFormat":47,"isAccessibleForFree":50,"interactionStatistic":51},"DigitalDocument",{"url":37,"@type":38,"width":39,"height":40},"https://docshare.wps.com/thumbnails/epigenetic-drugs-in-cancer-therapy/373036.png","ImageObject",300,407,{"name":42,"@type":43},"Liam","Person",{"url":19,"name":45,"@type":46},"DocShare","Organization","application/pdf","2026-10-29","2026-09-23",true,{"@type":52,"interactionType":53,"userInteractionCount":55},"InteractionCounter",{"@type":54},"ViewAction",12,{"@type":57,"mainEntity":58},"FAQPage",[59,65,69],{"name":60,"@type":61,"acceptedAnswer":62},"What are epigenetic modifications and how do they affect cancer-related processes?","Question",{"text":63,"@type":64},"Epigenetic modifications change chromatin structure and DNA accessibility, which affects DNA replication, DNA repair, and transcription. They are reversible and include DNA methylation and histone acetylation/methylation.","Answer",{"name":66,"@type":61,"acceptedAnswer":67},"Which classes of epigenetic drugs are discussed for cancer therapy?",{"text":68,"@type":64},"The review discusses inhibitors targeting epigenetic modifications: DNA methyltransferase inhibitors (DNMTi), histone deacetylase inhibitors (HDACi), histone methyltransferase inhibitors (HMTi), and bromodomain and extra-terminal motif protein inhibitors (BETi).",{"name":70,"@type":61,"acceptedAnswer":71},"How can epigenetic drugs be used to improve anti-tumor outcomes?",{"text":72,"@type":64},"The document highlights promising anti-cancer effects from combining epi-drugs with standard chemotherapeutic agents, and it also addresses delivery methods and tumor epigenetic biomarkers to reduce off-target toxicity and improve specificity.","https://schema.org",{"og:url":32,"og:type":75,"og:title":10,"og:site_name":45,"og:description":12},"article",{"robots":77,"canonical":32},"index,follow",{"doc_id":79,"site_id":7},373036,1790353066,{"code":4,"msg":82,"data":83},"success",[84,88,92,96,101,106,110,115,120,123,127],{"id":22,"doc_module":4,"doc_module_name":25,"category_name":85,"show_sort_weight":86,"slug":87},"Story & Novel",90,"story-novel",{"id":26,"doc_module":4,"doc_module_name":25,"category_name":89,"show_sort_weight":90,"slug":91},"Literature",80,"literature",{"id":33,"doc_module":4,"doc_module_name":25,"category_name":93,"show_sort_weight":94,"slug":95},"Exam",70,"exam",{"id":97,"doc_module":4,"doc_module_name":25,"category_name":98,"show_sort_weight":99,"slug":100},5,"Comic",60,"comic",{"id":102,"doc_module":4,"doc_module_name":25,"category_name":103,"show_sort_weight":104,"slug":105},6,"Technology",50,"technology",{"id":107,"doc_module":4,"doc_module_name":25,"category_name":29,"show_sort_weight":108,"slug":109},7,40,"healthcare",{"id":111,"doc_module":4,"doc_module_name":25,"category_name":112,"show_sort_weight":113,"slug":114},8,"Research & Report",30,"research-report",{"id":116,"doc_module":4,"doc_module_name":25,"category_name":117,"show_sort_weight":118,"slug":119},9,"Religion & Spirituality",20,"religion-spirituality",{"id":118,"doc_module":4,"doc_module_name":25,"category_name":121,"show_sort_weight":118,"slug":122},"World Cup","world-cup",{"id":124,"doc_module":4,"doc_module_name":25,"category_name":125,"show_sort_weight":124,"slug":126},10,"Lifestyle","lifestyle",{"id":128,"doc_module":4,"doc_module_name":25,"category_name":129,"show_sort_weight":97,"slug":130},19,"General","general",{"code":4,"msg":82,"data":132},{"doc_id":79,"user_id":133,"nickname":42,"user_avatar":134,"doc_module":4,"category_id":107,"category_name":29,"doc_title":10,"doc_description":12,"doc_content":135,"file_id":136,"file_url":137,"file_type":138,"file_size":139,"view_count":55,"is_deleted":4,"is_public":22,"is_downloadable":22,"audit_status":22,"page_count":140,"language":141,"language_code":8,"site_id":7,"html_lang":8,"table_of_contents":142,"faqs":143,"seo_title":144,"seo_description":12,"update_tm":145,"read_time":108},8796095461564,"https://ap-avatar.wpscdn.com/davatar_155a257f0dc6eb9ab79c44ca47cae57d","Cancer and Metastasis Reviews (2025) 44:37  \n[https://doi.org/10.1007/s10555-025-10253-7](https://doi.org/10.1007/s10555-025-10253-7)  \nEpigenetic drugs in cancer therapy  \nAmila Suraweera1 · Kenneth J. O’Byrne1,2 · Derek J. Richard1  \nReceived: 28 October 2024 / Accepted: 18 February 2025 / Published online: 26 February 2025 © The Author(s) 2025  \nAbstract  \nGenetic and epigenetic modifications of DNA are involved in cancer initiation and progression. Epigenetic modifications change chromatin structure and DNA accessibility and thus affect DNA replication, DNA repair and transcription. Epigenetic modifications are reversible and include DNA methylation, histone acetylation and histone methylation. DNA methylationis catalysed by DNA methyltransferases, histone acetylation and deacetylation are catalysed by histone acetylases and deacetylases, while histone methylation is catalysed by histone methyltransferases. Epigenetic modifications are dysregulated in several cancers, making them cancer therapeutic targets. Epigenetic drugs (epi-drugs) which are inhibitors of epigenetic modifications and include DNA methyltransferase inhibitors (DNMTi), histone deacetylase inhibitors (HDACi), histone methyltransferase inhibitors (HMTi) and bromodomain and extra-terminal motif protein inhibitors (BETi), have demonstrated clinical success as anti-cancer agents. Furthermore, the combination of epi-drugs with standard chemotherapeutic agents has demonstrated promising anti-cancer effects in pre-clinical and clinical settings. In this review, we discuss the role of epi-drugs in cancer therapy and explore their current and future use in combination with other anti-cancer agents used in the clinic. We further highlight the side effects and limitations of epi-drugs. We additionally discuss novel delivery methods and novel tumour epigenetic biomarkers for the screening, diagnosis and development of personalised cancer treatments, in order to reduce off-target toxicity and improve the specificity and anti-tumour efficacy of epi-drugs.  \nKeywords Epigenetic drugs · Cancer therapy · DNA methyltransferase inhibitors · Histone deacetylase inhibitors · Histone methyltransferase inhibitors  \n1 Introduction  \nThe term epigenetics was first coined in 1942 by Conrad Waddington to establish a connection between the genotype and phenotype [1, 2] . Today, the term epigenetics refers to the study of reversible heritable changes in gene expression that are not due to alterations in the DNA sequence [3, 4] . Epigenetic modifications change DNA accessibility and thereby affect transcription, DNA replication and DNA repair. The main epigenetic mechanisms include histone modifications, DNA methylation, chromatin remodelling and  \n* Amila Suraweera[amila.suraweera@qut.edu.au](amila.suraweera@qut.edu.au)  \n1 School of Biomedical Sciences, Centre for Genomicsand Personalised Health, Queensland University of Technology (QUT), 60 Musk Avenue, Kelvin Grove, QLD 4059, Australia  \n2 Princess Alexandra Hospital, 199 Ipswich Road, Woolloongabba, QLD 4102, Australia  \nnon-coding RNA [3, 5, 6] . Histones are central components of chromatin which can be covalently modified. Histone N-terminal post-translational modifications include methylation, acetylation, phosphorylation, ubiquitination, sumoylation, ADP ribosylation, citrullination, proline isomerization, beta-N-acetylglucosamine and lactylation [7 , 8] . The two most abundant and widely studied histone post-translational modifications include acetyl and methyl groups. While acetylated histones are less compact and facilitate transcription, methylated histones can be activating or repressive. DNA methyltransferases (DNMT) catalyse DNA methylation, histone acetyltransferases (HAT) add acetyl groups to histones, histone deacetylases (HDAC) remove acetyl groups, histone methyltransferases (HMT) catalyse histone methylation and histone demethylases catalyse the removal of methyl groups from arginine and lysine residues on histone","cbCaihSh9OGCdpbB","https://ap.wps.com/l/cbCaihSh9OGCdpbB","pdf",912201,16,"English","# Abstract\n# Introduction\n## Epigenetics and epigenetic mechanisms\n## Epigenetic dysregulation in cancer and therapeutic targets\n## FDA-approved epigenetic drugs and BET inhibitors","[{\"question\":\"What are epigenetic modifications and how do they affect cancer-related processes?\",\"answer\":\"Epigenetic modifications change chromatin structure and DNA accessibility, which affects DNA replication, DNA repair, and transcription. They are reversible and include DNA methylation and histone acetylation/methylation.\"},{\"question\":\"Which classes of epigenetic drugs are discussed for cancer therapy?\",\"answer\":\"The review discusses inhibitors targeting epigenetic modifications: DNA methyltransferase inhibitors (DNMTi), histone deacetylase inhibitors (HDACi), histone methyltransferase inhibitors (HMTi), and bromodomain and extra-terminal motif protein inhibitors (BETi).\"},{\"question\":\"How can epigenetic drugs be used to improve anti-tumor outcomes?\",\"answer\":\"The document highlights promising anti-cancer effects from combining epi-drugs with standard chemotherapeutic agents, and it also addresses delivery methods and tumor epigenetic biomarkers to reduce off-target toxicity and improve specificity.\"}]","Epigenetic drugs in cancer therapy | PDF",1790196417]