College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, China.
The Second Affiliated Hospital of Jiaxing University, Jiaxing, China.
Curr Med Chem. 2020;27(33):5530-5542. doi: 10.2174/0929867326666190528080514.
Mixed Lineage Leukemia 1 (MLL1), an important member of Histone Methyltransferases (HMT) family, is capable of catalyzing mono-, di-, and trimethylation of Histone 3 lysine 4 (H3K4). The optimal catalytic activity of MLL1 requires the formation of a core complex consisting of MLL1, WDR5, RbBP5, and ASH2L. The Protein-Protein Interaction (PPI) between WDR5 and MLL1 plays an important role in abnormal gene expression during tumorigenesis, and disturbing this interaction may have a potential for the treatment of leukemia harboring MLL1 fusion proteins. In this review, we will summarize recent progress in the development of inhibitors targeting MLL1- WDR5 interaction.
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、二和三甲基化。MLL1 的最佳催化活性需要形成一个核心复合物，该复合物由 MLL1、WDR5、RbBP5 和 ASH2L 组成。WDR5 和 MLL1 之间的蛋白-蛋白相互作用（PPI）在肿瘤发生过程中的异常基因表达中起着重要作用，干扰这种相互作用可能具有治疗携带 MLL1 融合蛋白的白血病的潜力。在这篇综述中，我们将总结靶向 MLL1-WDR5 相互作用抑制剂的最新进展。
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