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

doi:10.2174/0929867326666190528080514

	The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction
	Ye, Xiaoqing 2,3; Chen, Gang 1; Jin, Jia 2; Zhang, Binzhong 1; Wang, Yinda 1; Cai, Zhenhai 1; Ye, Fei 2
刊名	CURRENT MEDICINAL CHEMISTRY
	2020
卷号	27 期号:33 页码:5530-5542
关键词	WDR5 MLL1 histone methyltransferase small-molecular inhibitor epigenetics human acute leukemia
ISSN号	0929-8673
DOI	10.2174/0929867326666190528080514
通讯作者	Ye, Fei(yefei@zstu.edu.cn)
英文摘要	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.
资助项目	Natural Science Foundation of Zhejiang Province[LY18H300008] ; National Natural Science Foundation of China[81803339]
WOS关键词	H3K4 METHYLTRANSFERASE ACTIVITY ; STRUCTURE-BASED DESIGN ; AIDED DRUG DESIGN ; HISTONE H3 ; MOLECULAR RECOGNITION ; STRUCTURAL BASIS ; HIGH-AFFINITY ; SET1 FAMILY ; MLL PROTEIN ; COMPLEX
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000580568500004
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/291486]
专题	中国科学院上海药物研究所
通讯作者	Ye, Fei
作者单位	1.Jiaxing Univ, Affiliated Hosp 2, Jiaxing, Peoples R China 2.Zhejiang Sci Tech Univ, Coll Life Sci & Med, Hangzhou, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Ye, Xiaoqing,Chen, Gang,Jin, Jia,et al. The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction[J]. CURRENT MEDICINAL CHEMISTRY,2020,27(33):5530-5542.
APA	Ye, Xiaoqing.,Chen, Gang.,Jin, Jia.,Zhang, Binzhong.,Wang, Yinda.,...&Ye, Fei.(2020).The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction.CURRENT MEDICINAL CHEMISTRY,27(33),5530-5542.
MLA	Ye, Xiaoqing,et al."The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction".CURRENT MEDICINAL CHEMISTRY 27.33(2020):5530-5542.