Submit Manuscript  

Article Details


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

[ Vol. 27 , Issue. 33 ]

Author(s):

Xiaoqing Ye, Gang Chen, Jia Jin, Binzhong Zhang, Yinda Wang, Zhenhai Cai and Fei Ye*   Pages 5530 - 5542 ( 13 )

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:

WDR5, MLL1, histone methyltransferase, small-molecular inhibitor, epigenetics, human acute leukemia.

Affiliation:

College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, The Second Affiliated Hospital of Jiaxing University, Jiaxing, College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, The Second Affiliated Hospital of Jiaxing University, Jiaxing, The Second Affiliated Hospital of Jiaxing University, Jiaxing, The Second Affiliated Hospital of Jiaxing University, Jiaxing, College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou



Read Full-Text article