Design and synthesis of benzylpiperidine inhibitors targeting the menin-MLL1 interface
文献类型：期刊论文
| 作者 | Ren, Jing2,3; Xu, Wei1,2; Tang, Le3; Su, Minbo1; Chen, Danqi3 ; Chen, Yue-Lei2,3; Zang, Yi1; Li, Jia1,2; Shen, Jingkang2,3; Zhou, Yubo1,2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2016-09-15 |
| 卷号 | 26期号:18页码:4472-4476 |
| 关键词 | Menin Mixed lineage leukemia MLL1 SAR Inhibitor |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.07.074 |
| 文献子类 | Article |
| 英文摘要 | Menin is an essential oncogenic cofactor for mixed lineage leukemia (MLL)-mediated leukemogenesis, functioning through its direct interaction with MLL1 protein. Therefore, targeting the menin-MLL1 protein-protein interface represents a promising strategy to block MLL-mediated leukemogenesis. On the basis of co-crystal structure analysis, starting from thienopyrimidine chemotype, we have investigated the detailed structure-activity relationship of the piperazinyl-dihydrothiazole moiety. Several compounds were found with potent inhibitory activity against menin and better activities in cell-based experiments than MI-2-2. Molecular docking analysis revealed a less explored subpocket, which could be used for the design of new menin-MLL1 inhibitors. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MIXED LINEAGE LEUKEMIA ; PROTEIN-PROTEIN INTERACTION ; MLL INTERACTION ; TRANSFORMATION ; GENE ; REARRANGEMENTS ; EXPRESSION ; HOXA9 |
| 资助项目 | National Natural Science Foundation of China[81273368] ; National Natural Science Foundation of China[81330076] ; National Natural Science Foundation of China[81473094] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program' of China[2014ZX09507-002] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program' of China[2013ZX09507001] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000382263800017 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275889]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Zhou, Yubo; Xiong, Bing |
| 作者单位 | 1.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China; 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Ren, Jing,Xu, Wei,Tang, Le,et al. Design and synthesis of benzylpiperidine inhibitors targeting the menin-MLL1 interface[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(18):4472-4476. |
| APA | Ren, Jing.,Xu, Wei.,Tang, Le.,Su, Minbo.,Chen, Danqi.,...&Xiong, Bing.(2016).Design and synthesis of benzylpiperidine inhibitors targeting the menin-MLL1 interface.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(18),4472-4476. |
| MLA | Ren, Jing,et al."Design and synthesis of benzylpiperidine inhibitors targeting the menin-MLL1 interface".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.18(2016):4472-4476. |
入库方式： OAI收割
来源：上海药物研究所
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