文献类型： 外文期刊

第一作者： Yi-Chao Zheng

作者： Yi-Chao Zheng;Jiao Chang;Lin-Chen Wang;Hong-Mei Ren;Jing-Ru Pang;Hong-Min Liu

作者机构：

关键词： KDM5B; Cancer; Inhibitor; Histone modification

期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.514； 五年影响因子：6.099 ）

ISSN： 0223-5234

年卷期： 2019 年 161 卷

页码：

收录情况： SCI

摘要： Lysine demethylase 513 (KDM5B) is a histone demethylase identified in 2007, which is responsible for erasing H3K4me2/3 activation marker. It participates in multiple repressive transcriptional complexes around target gene promoters and performs wide regulatory effects on chromatin structure. Until now, there is growing evidence for the oncogenic function of KDM5B. As the H3K4me2/3 residue represents the transcription initiation site of the active transcription gene, and demethylation of H3K4 is associated with transcriptional repression, making it a potential participant in inhibiting the expression of tumor suppressors. Therefore, KDM5B is considered as a promising drug target for cancer therapy, and many medicinal chemists are trying to design and synthesize potent and selective KDM5B inhibitors with the aid of high-throughput screening, structure based drug design, and structure activity relationship studies. This review focuses on the basic biochemical and physiological function of KDM5B and its involved mechanisms in cancers, a comprehensive overview of KDM5B inhibitors is also introduced. (C) 2018 Elsevier Masson SAS. All rights reserved.

分类号：