组蛋白去甲基化酶JMJD及其抑制剂的研究进展

Research Progress of Histone Demethylase JMJD and Its Inhibitors

组蛋白去甲基化酶JMJD家族可通过催化去除组蛋白N末端赖氨酸残基上甲基,参与表观遗传调控,包括基因表达调控,并与某些疾病,特别是癌症密切相关。因此,该酶已成为令人关注的癌症治疗新靶点,其抑制剂也成为药物研究与开发的热点。综述JMJD与肿瘤的关联、JMJD的结构和催化机制及其抑制剂的研究进展。

Histone demethvlase JMJD thmily has been found to be involved in epigenetic regulation including gene expression regulation bycatalyzing to remove methyl groups from lysine residues of the N-terminal tails of histones and to be closely related to several diseases, especiallycancer. Theretbre, the enzyme has been considered as a new therapeutic target for cancer and the research and development of its inhibitors have also become a hot topic. The research progress on the association of JMJD with tumor, the structure and catalytic mechanism of JMJD and its mhibitors was reviewed.