| DNA去甲基化药物的研究进展 |
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| 引用本文： | 许嵘,张文州,辛军,陈琳琳,丁小明,谢志新,林阳君,唐生安.DNA去甲基化药物的研究进展[J].现代药物与临床,2017,32(1):158-164. |
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| 作者姓名： | 许嵘 张文州 辛军 陈琳琳 丁小明 谢志新 林阳君 唐生安 |
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| 作者单位： | 1. 泉州医学高等专科学校 药学院，福建 泉州 362011; 南加州大学 凯克医学中心 诺里斯综合癌症中心，美国 洛杉矶 90089;2. 泉州医学高等专科学校 药学院,福建 泉州,362011;3. 福建医科大学附属泉州第一医院 泌尿外科,福建 泉州,362000;4. 天津医科大学 药学院 天津市临床药物关键技术重点实验室,天津,300070 |
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| 基金项目： | 中国博士后基金资助项目（2016M591399）；福建省中青年教师教育科研项目（JAT160852）；天津市自然科学基金重点项目（16JCZDJC32600） |
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| 摘 要： | DNA甲基化是调节基因表达而不改变DNA碱基序列的表观遗传修饰,通过沉默肿瘤抑制基因在癌症发展中发挥关键作用。DNA去甲基化药物在临床上已经显示出疗效,然而,高效性和特异性的DNA去甲基化药物尚未出现。目前,在市场上已有2种药物阿扎胞苷和地西他滨用于治疗骨髓增生异常综合征。寻找直接结合靶点新的抑制剂是未来的方向。从抗肿瘤活性和临床研究方面介绍了DNA去甲基化药物的研究进展。
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| 关 键 词： | DNA甲基化 DNA去甲基化药物 阿扎胞苷 地西他滨 天然产物 癌症 |
| 收稿时间： | 2016/10/31 0:00:00 |
Research progress on DNA demethylating agents |
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| XU Rong,ZHANG Wen-zhou,XIN Jun,CHEN Lin-lin,DING Xiao-ming,XIE Zhi-xin,LIN Yang-jun and TANG Sheng-an.Research progress on DNA demethylating agents[J].Drugs & Clinic,2017,32(1):158-164. |
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| Authors: | XU Rong ZHANG Wen-zhou XIN Jun CHEN Lin-lin DING Xiao-ming XIE Zhi-xin LIN Yang-jun and TANG Sheng-an |
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| Institution: | School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;Norris Comprehensive Cancer Center, Keck School of Medicine, University of Southern California, Los Angeles 90089, USA;School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;Department of Urology, the First Hospital of Quanzhou Affiliated Fujian Medical University, Quanzhou 362000, China;School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;School of Pharmacy, Quanzhou Medical College, Quanzhou 362011, China;Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics(Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China |
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| Abstract: | DNA methylation is an epigenetic modification that modulates gene expression without altering the DNA base sequence, which plays a crucial role in cancer by silencing tumor suppressor genes. DNA demethylating agents have shown efficacy in clinics. However, highly efficient and specific DNA demethylating agents have not yet been found. At present, two drugs, azacitidine and decitabine are on the market for the treatment of myelodysplastic syndrome. Improving methods will certainly lead to the prediction of novel directly binding inhibitors in the future. This article reviewed the progress on antitumor activities and clinical studies of DNA demethylating agents. |
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| Keywords: | DNA methylation DNA demethylating agents azacitidine decitabine natural products cancer |
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