Review Article

含溴结构域蛋白4:可药物治疗的目标

卷 20, 期 15, 2019

页: [1517 - 1536] 页: 20

弟呕挨: 10.2174/1574885514666190618113519

价格: $65

摘要

含溴结构域的蛋白质4(BRD4)属于溴结构域和末端外家族。 BRD4抑制剂可以调节乙酰化的赖氨酸并形成蛋白质复合物,从而启动转录程序,作为组蛋白代码的表观遗传调节剂。 最初,BRD4被认为是对抗恶性肿瘤最有希望的靶标之一。 但是,最近的许多研究表明,BRD4在多种疾病(包括癌症,冠心病,神经系统疾病和肥胖症)中起着至关重要的作用。 目前,几种BRD4抑制剂正在接受临床试验。 寻找新的BRD4抑制剂似乎对于开发新药具有很大的实用性。 在此小型审查中,我们重点介绍了来自天然产物和合成来源的BRD4抑制剂,及其在癌症,糖脂代谢,炎症,神经元刺激激活,人类免疫缺陷病毒和肾纤维化中的应用。

关键词: 含溴结构域的蛋白质4,小分子抑制剂,药理学,肿瘤,冠心病,天然产物,合成化合物。

图形摘要

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