| BET bromodomain蛋白小分子抑制剂研究进展 |
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| 引用本文： | 柳克俊,张智敏,冉挺,陈红丽,陆涛,陈亚东.BET bromodomain蛋白小分子抑制剂研究进展[J].中国药科大学学报,2015,46(3):264-271. |
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| 作者姓名： | 柳克俊 张智敏 冉挺 陈红丽 陆涛 陈亚东 |
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| 作者单位： | 中国药科大学理学院;中国药科大学理学院;中国药科大学理学院;中国药科大学理学院;中国药科大学理学院;中国药科大学理学院 |
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| 基金项目： | 国家自然科学基金资助项目(No.81473077/H3001)；江苏省高校“青蓝工程”资助项目；江苏省普通高校研究生科研创新计划(No.CXZZ13_0337) |
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| 摘 要： | 组蛋白赖氨酸乙酰化的识别是组蛋白乙酰化参与表观遗传调控的关键步骤,乙酰化的组蛋白赖氨酸可以被bromodomains(BRDs)结构域所特异性的识别,从而招募染色质调控因子到特定区域,协同完成基因表达调控。其中作用于bromodomain and extra-terminal(BET)蛋白家族的BRD结构域的小分子抑制剂在抗炎和抗肿瘤方面显示出巨大的潜力。本文通过对与BET bromodomain靶点相关的疾病、BET bromodomain结构、BET bromodomain小分子抑制剂的化学结构分类及其构效关系等多方面进行总结,为设计和开发高活性的BET bromodomain小分子抑制剂提供参考依据。
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| 关 键 词： | BET bromodomain 小分子抑制剂 肿瘤 进展 |
Advances in BET bromodomain protein inhibitors |
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| LIU Kejun,ZHANG Zhimin,RAN Ting,CHEN Hongli,LU Tao and CHEN Yadong.Advances in BET bromodomain protein inhibitors[J].Journal of China Pharmaceutical University,2015,46(3):264-271. |
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| Authors: | LIU Kejun ZHANG Zhimin RAN Ting CHEN Hongli LU Tao and CHEN Yadong |
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| Institution: | LIU Kejun;ZHANG Zhimin;RAN Ting;CHEN Hongli;LU Tao;CHEN Yadong;School of Sciences,China Pharmaceutical University; |
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| Abstract: | Recognizing acetyl-lysine of histone is a key process of epigenetic regulation that is mediated by a protein module called bromodomain(BRD). The bromodomain inhibitors of the bromodomains and extra-terminal(BET)family have shown great potential in anti-inflammatory and antiproliferative effects. Through a review of diseases and structures about BET bromodomain, different kinds of inhibitors were analyzed and their structure-activity relationships were summarized. Herenin, the recent advances reported are reviewed for discovering more excellent small molecule inhibitors. |
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| Keywords: | BET bromodomain small molecular inhibitors tumor advances |
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