Design and synthesis of benzylpiperidine inhibitors targeting the menin-mll1 interface
文献类型：期刊论文
| 作者 | Ren, Jing1,3; Xu, Wei2,3; Tang, Le1; Su, Minbo2; Chen, Danqi1; Chen, Yue-Lei1,3; Zang, Yi2; Li, Jia2,3; Shen, Jingkang1,3; Zhou, Yubo2,3 |
| 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 |
| 通讯作者 | Zhou, yubo(ybzhou@simm.ac.cn) ; Xiong, bing(bxiong@simm.ac.cn) |
| 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 |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| WOS类目 | Chemistry, Medicinal ; Chemistry, Organic |
| 语种 | 英语 |
| WOS记录号 | WOS:000382263800017 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2375634 |
| 专题 | 中国科学院大学 |
| 通讯作者 | Zhou, Yubo; Xiong, Bing |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, 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. |
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来源：中国科学院大学
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