| 组蛋白去甲基化酶JMJD 及其抑制剂的研究进展 |
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| 引用本文： | 王海,冯涛涛,孙昊鹏,尤启东.组蛋白去甲基化酶JMJD 及其抑制剂的研究进展[J].微生物学杂志,2013(11). |
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| 作者姓名： | 王海 冯涛涛 孙昊鹏 尤启东 |
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| 作者单位： | 中国药科大学药物化学教研室，江苏 南京 210009,中国药科大学药物化学教研室，江苏 南京 210010,中国药科大学药物化学教研室，江苏 南京 210011,中国药科大学药物化学教研室，江苏 南京 210012 |
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| 基金项目： | 国家科技重大专项“企业创新药物孵化基地”项目（No.2012ZX09401） |
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| 摘 要： | 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。
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| 关 键 词： | 组蛋白去甲基化酶 JMJD JMJD抑制剂 肿瘤 |
Research Progress of Histone Demethylase JMJD and |
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| WANG Hai,FENG Taotao,SUN Haopeng and YOU Qidong.Research Progress of Histone Demethylase JMJD and[J].Journal of Microbiology,2013(11). |
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| Authors: | WANG Hai FENG Taotao SUN Haopeng and YOU Qidong |
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| Institution: | Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009,China,Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210010,China,Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210011,China and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210012,China |
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| Abstract: | Histone demethylase JMJD family has been found to be involved in epigenetic regulation including gene expression regulation by catalyzing to remove methyl groups from lysine residues of the N-terminal tails of histones and to be closely related to several diseases, especially cancer. Therefore, 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 inhibitors was reviewed. |
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| Keywords: | histone demethylase JMJD JMJD inhibitor tumor |
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