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

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

Xiaoqing Ye, Gang Chen, Jia Jin, Binzhong Zhang, Yinda Wang, Fei Ye

Curr Med Chem. 2019 May 27.

PMID: 31132972

Abstract:

Mixed lineage leukemia 1 (MLL1), an important member of histone methyltransferases (HMT) family, is closely associated with human acute leukemia. MLL1 could specially catalyze mono-, di-, and trimethylation of histone 3 lysine 4 (H3K4) via its conserved SET domain, the proper enzymatic activity depends on a core complex consisting of MLL1, WDR5, RbBP5, ASH2L and Dpy30. The protein-protein interaction (PPI) between WDR5 and MLL1 plays an important role in abnormal gene expression during tumorigenesis, disturbing MLL1-WDR5 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 on inhibitors targeting MLL1-WDR5 interaction.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR42416111	MLL1/WDR5/Ash2L/RbBP5 human			Price
IAR42416122	DPY30 human			Price

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