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Review Article

肿瘤治疗中溴结构域和外末端结构域蛋白的靶向研究进展

卷 29, 期 25, 2022

发表于: 28 March, 2022

页: [4391 - 4409] 页: 19

弟呕挨: 10.2174/0929867329666220211091806

价格: $65

摘要

溴化结构域和末端外结构域（BET）蛋白是一个被广泛研究的与多种疾病相关的蛋白家族，包括恶性肿瘤和慢性炎症。目前，许多pan BET抑制剂已经在多个体内临床前模型中显示出了强大的疗效，并进入临床试验，但由于不良事件而在很大程度上停滞不前。因此，迫切需要开发新的靶向BET的选择性抑制剂和蛋白水解靶向嵌合体 （Proteolysis Targeting Chimeras, PROTACs）。本文综述了BET蛋白的结构和近年来BET抑制剂的研究进展，重点介绍了BRD4选择性抑制剂和PROTAC降解物。

关键词: 癌症，BET, BRD4，抑制剂，PROTAC，药物设计。

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