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Review Article

针对混合谱系白血病1（MLL1）-WD重复域5蛋白（WDR5）蛋白质-蛋白质相互作用的抑制剂的开发

卷 27, 期 33, 2020

页: [5530 - 5542] 页: 13

弟呕挨: 10.2174/0929867326666190528080514

价格: $65

摘要

混合谱系白血病1（MLL1）是组蛋白甲基转移酶（HMT）家族的重要成员，能够催化组蛋白3赖氨酸4（H3K4）的单甲基，二甲基和三甲基化。 MLL1的最佳催化活性需要形成由MLL1，WDR5，RbBP5和ASH2L组成的核心配合物。 WDR5和MLL1之间的蛋白质相互作用（PPI）在肿瘤发生过程中的异常基因表达中起重要作用，并且干扰这种相互作用可能对具有MLL1融合蛋白的白血病具有潜在的治疗作用。 在这篇综述中，我们将总结靶向MLL1-WDR5相互作用的抑制剂的最新进展。

关键词: WDR5，MLL1，组蛋白甲基转移酶，小分子抑制剂，表观遗传学，人类急性白血病。

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