摘要
可逆的组蛋白甲基化是一种重要的表观遗传调控方式。组蛋白赖氨酸的甲基化由组蛋白赖氨酸甲基转移酶(HKMTs)和组蛋白赖氨酸去甲基化酶(HKDMs)动态调节。HKDMs的异常调节与多种癌症(包括乳腺癌)的发生发展及耐药密切相关。HKDMs小分子抑制剂既可以作为抗肿瘤药物用于治疗癌症,又可以作为化学探针来研究表观遗传学,因此对其开发具有重要意义。本文就HKDMs在乳腺癌中的作用和HKDMs抑制剂及其临床应用潜力展开综述。
Reversible histone methylation is an important epigenetic regulation. Histone lysine methylation is dynamically controlled by histone lysine methyltransferases（HKMTs） and histone lysine demethylases（HKDMs）. The dysregulation of HKDMs is closely related to the carcinogenesis and development of numerous cancers, including breast cancer, and drug resistance. Small molecular inhibitors of HKDMs could be used as antitumor drugs for cancer therapy, or as chemical probes for investigation of epigenetics. It is of great significance to discover and develop HKDMs inhibitors. In this review, we summarize the roles of histone lysine demethylases in breast cancer, as well as HKDMs inhibitors and their clinical application potency.
作者
刘丹
邵阳光
LIU Dan1, SHAO Yangguang2.(1Seven-year-program of Clinical Medicine, China Medical University, Shenyang 110122, China; 2Department of Molecular Cell Biology, Key Laboratory of Cell Biology, National Health and Family Planning Commission, and Key Laboratory of Medical Cell Biology, Ministry of Education, China Medical University, Shenyang 110122, Chin)
出处
《生命的化学》
CAS
CSCD
2018年第1期47-54,共8页
Chemistry of Life
基金
国家自然科学基金项目(31271389)
2017年辽宁省大学生创新创业训练计划项目(201710159000127)
