The Development of Inhibitors Targeting the Mixed Lineage Leukemia 1 (MLL1)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction
文献类型：期刊论文
| 作者 | Ye, Xiaoqing2,3; Chen, Gang1; Jin, Jia3; Zhang, Binzhong1; Wang, Yinda1; Cai, Zhenhai1; Ye, Fei3 |
| 刊名 | CURRENT MEDICINAL CHEMISTRY
 |
| 出版日期 | 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. |
| 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 |
| 资助项目 | Natural Science Foundation of Zhejiang Province[LY18H300008] ; National Natural Science Foundation of China[81803339] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000580568500004 |
| 出版者 | BENTHAM SCIENCE PUBL LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/291486]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Ye, Fei |
| 作者单位 | 1.Jiaxing Univ, Affiliated Hosp 2, Jiaxing, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China 3.Zhejiang Sci Tech Univ, Coll Life Sci & Med, Hangzhou, 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. |
入库方式： OAI收割
来源：上海药物研究所
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