{"title":"Current advances and future directions in targeting histone demethylases for cancer therapy","authors":"June-Ha Shin , Hye-Been Yoo , Jae-Seok Roe","doi":"10.1016/j.mocell.2025.100192","DOIUrl":null,"url":null,"abstract":"<div><div>Epigenetic regulators, known as “writers,” erasers,” and “readers,” are essential for controlling gene expression by adding, removing, or recognizing post-translational modifications to histone tails, respectively. These regulators significantly affect genes involved in cancer initiation and maintenance. Recently, several clinical strategies targeting these epigenetic enzymes have emerged and some trials have demonstrated promising results for cancer treatment. Histone lysine demethylases (KDMs) yield distinct transcriptional outcomes that depend on the position of the methylated lysine and the specific genotype or lineage of the cancer cells. Due to their diverse roles in transcription, KDMs offer valuable opportunities for precision oncology, allowing treatments to be tailored to meet individual patient needs. This review emphasizes our current understanding of the functional relationship between KDMs and cancer as well as the development and application of small-molecule compounds that target KDMs.</div></div>","PeriodicalId":18795,"journal":{"name":"Molecules and Cells","volume":"48 3","pages":"Article 100192"},"PeriodicalIF":6.5000,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecules and Cells","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1016847825000160","RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/2/10 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Epigenetic regulators, known as “writers,” erasers,” and “readers,” are essential for controlling gene expression by adding, removing, or recognizing post-translational modifications to histone tails, respectively. These regulators significantly affect genes involved in cancer initiation and maintenance. Recently, several clinical strategies targeting these epigenetic enzymes have emerged and some trials have demonstrated promising results for cancer treatment. Histone lysine demethylases (KDMs) yield distinct transcriptional outcomes that depend on the position of the methylated lysine and the specific genotype or lineage of the cancer cells. Due to their diverse roles in transcription, KDMs offer valuable opportunities for precision oncology, allowing treatments to be tailored to meet individual patient needs. This review emphasizes our current understanding of the functional relationship between KDMs and cancer as well as the development and application of small-molecule compounds that target KDMs.
期刊介绍：
Molecules and Cells is an international on-line open-access journal devoted to the advancement and dissemination of fundamental knowledge in molecular and cellular biology. It was launched in 1990 and ISO abbreviation is "Mol. Cells". Reports on a broad range of topics of general interest to molecular and cell biologists are published. It is published on the last day of each month by the Korean Society for Molecular and Cellular Biology.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
