含溴结构域和额外终端域家族蛋白——表观遗传领域的新型治疗靶点
发布时间：2018-10-08 11:47
【摘要】：BET(bromodomain and extraterminal)是一类能解读表观遗传密码的蛋白,通过识别和结合乙酰化的组蛋白或非组蛋白,在调节基因转录中发挥重要的作用。BET抑制剂在肿瘤和炎症等临床前疾病模型中表现出良好的疗效,且已有部分抑制剂进入临床阶段,这表明以BET为治疗靶点的药物研发具有可观前景。本文将对BET蛋白的结构功能、BET抑制剂与疾病治疗以及其作为治疗靶点的分子机制等方面进行阐述。
[Abstract]:BET (bromodomain and extraterminal) is a class of proteins that can interpret epigenetic codes by recognizing and binding acetylated histone or non-histone. BET inhibitors play an important role in regulating gene transcription. BET inhibitors have shown good efficacy in preclinical disease models such as tumor and inflammation, and some inhibitors have entered the clinical stage. This suggests that drug development with BET as a therapeutic target has a promising future. In this paper, the structure and function of BET protein, its inhibitor and disease treatment, and its molecular mechanism as therapeutic targets are reviewed.
【作者单位】： 美国伊利诺伊大学香槟分校生化系;中国医学科学院北京协和医学院医药生物技术研究所;
【基金】：基金项目:中国医学科学院医学与健康科技创新工程(2016-I2M-2-002)
【分类号】：R96
，
本文编号：2256628
[Abstract]:BET (bromodomain and extraterminal) is a class of proteins that can interpret epigenetic codes by recognizing and binding acetylated histone or non-histone. BET inhibitors play an important role in regulating gene transcription. BET inhibitors have shown good efficacy in preclinical disease models such as tumor and inflammation, and some inhibitors have entered the clinical stage. This suggests that drug development with BET as a therapeutic target has a promising future. In this paper, the structure and function of BET protein, its inhibitor and disease treatment, and its molecular mechanism as therapeutic targets are reviewed.
【作者单位】： 美国伊利诺伊大学香槟分校生化系;中国医学科学院北京协和医学院医药生物技术研究所;
【基金】：基金项目:中国医学科学院医学与健康科技创新工程(2016-I2M-2-002)
【分类号】：R96
，
本文编号：2256628
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