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Review
. 2020;27(33):5530-5542.
doi: 10.2174/0929867326666190528080514.

The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein- Protein Interaction

Xiaoqing Ye  1 , Gang Chen  2 , Jia Jin  1 , Binzhong Zhang  2 , Yinda Wang  2 , Zhenhai Cai  2 , Fei Ye  1
Affiliations
Review

The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein- Protein Interaction

Xiaoqing Ye et al. Curr Med Chem. 2020.

Abstract

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.

Keywords: MLL1; WDR5; epigenetics; histone methyltransferase; human acute leukemia; small-molecular inhibitor.

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