Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2
文献类型：期刊论文
| 作者 | Devkota, Kanchan1,4; Lohse, Brian4; Liu, Qing2,3; Wang, Ming-Wei2,3 ; Staerk, Dan4; Berthelsen, Jens1; Clausen, Rasmus Praetorius4
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2014-04 |
| 卷号 | 5期号:4页码:293-297 |
| 关键词 | Sinefungin methyltransferase inhibitors EHMT1 EHMT2 |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/ml4002503 |
| 文献子类 | Article |
| 英文摘要 | A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward Ado Met. |
| WOS关键词 | SUBTELOMERIC DELETION SYNDROME ; HISTONE METHYLTRANSFERASE G9A ; C-6 EPIMER ; METHYLATION ; CELLS |
| 资助项目 | University of Copenhagen[00000000] ; Danish Cancer Society[00000000] ; University of Copenhagen Programme of Excellence[00000000] ; Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2012ZX09304011] ; Ministry of Science and Technology of China[2013ZX09507002] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000334571400004 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277132]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Berthelsen, Jens |
| 作者单位 | 1.Univ Copenhagen, NNF Ctr Prot Res, DK-2200 Copenhagen, Denmark; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 4.Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark; |
| 推荐引用方式 GB/T 7714 | Devkota, Kanchan,Lohse, Brian,Liu, Qing,et al. Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2[J]. ACS MEDICINAL CHEMISTRY LETTERS,2014,5(4):293-297. |
| APA | Devkota, Kanchan.,Lohse, Brian.,Liu, Qing.,Wang, Ming-Wei.,Staerk, Dan.,...&Clausen, Rasmus Praetorius.(2014).Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.ACS MEDICINAL CHEMISTRY LETTERS,5(4),293-297. |
| MLA | Devkota, Kanchan,et al."Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2".ACS MEDICINAL CHEMISTRY LETTERS 5.4(2014):293-297. |
入库方式： OAI收割
来源：上海药物研究所
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