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Updated: Jan 24, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5)

Xiaoqing Ye1, Gang Chen2, Jia Jin1

  • 1College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, China.

Current Medicinal Chemistry
|May 29, 2019
PubMed

Insights

Targeting the Mixed Lineage Leukemia 1 (MLL1) and WDR5 protein interaction shows promise for treating MLL1-related leukemias. This review covers recent advancements in developing inhibitors for this crucial interaction.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Mixed Lineage Leukemia 1 (MLL1) is a key Histone Methyltransferase (HMT) catalyzing Histone 3 lysine 4 (H3K4) methylation.
  • MLL1's catalytic activity depends on a core complex including MLL1, WDR5, RbBP5, and ASH2L.
  • The MLL1-WDR5 Protein-Protein Interaction (PPI) is implicated in aberrant gene expression driving tumorigenesis.

Purpose of the Study:

  • To review recent progress in developing inhibitors targeting the MLL1-WDR5 interaction.
  • To explore the therapeutic potential of disrupting this PPI in leukemia treatment.

Main Methods:

  • Literature review of recent studies on MLL1-WDR5 inhibitors.
  • Analysis of the role of MLL1-WDR5 interaction in leukemia pathogenesis.

Main Results:

  • Several inhibitors targeting the MLL1-WDR5 interaction have been developed.
  • These inhibitors show potential for treating leukemias with MLL1 alterations.

Conclusions:

  • Disrupting the MLL1-WDR5 interaction is a viable therapeutic strategy for MLL1-driven leukemias.
  • Further research into MLL1-WDR5 inhibitors is warranted for leukemia treatment.
Keywords:
MLL1WDR5epigeneticshistone methyltransferasehuman acute leukemiasmall-molecular inhibitor

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