The mimics of N-epsilon-acyl-lysine derived from cysteine as sirtuin inhibitors
文献类型：期刊论文
| 作者 | Wang, Chun1; Wang, Fang1; Chen, Xiaoxue1; Zou, Yefang1; Zhu, Hong1; Zhao, Qingjie2 ; Shen, Jingshan2; Li, Yan1; Li, Yongjun1; He, Bin1,2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2018-08-01 |
| 卷号 | 28期号:14页码:2375-2378 |
| ISSN号 | 0960-894X |
| 关键词 | L-Cysteine The mimics of lysine Mechanism-based inhibitors Sirtuin inhibitors SIRT2 inhibitors |
| DOI | 10.1016/j.bmcl.2018.06.030 |
| 文献子类 | Article |
| 英文摘要 | Sirtuin inhibitors as physiological research tools and therapeutic potentials have caught many attentions in last decades. The mimics of acyl lysine have been approved to be a very efficient strategy for development of mechanism-based sirtuin inhibitors. In current study, a novel scaffold of L-S-(3-carboxamidopropyl) cysteine (LCAPC) has been exploited for design and synthesis of sirtuin inhibitors. As a result, the mimics of Ne-acyl-lysine derived from cysteine including small molecules (5a-m) and peptides (9a-m) have been synthesized. Among these, the peptides 9g and 9h were found to be the most inhibitory potency and selectivity against SIRT2. |
| WOS关键词 | ACETYL-LYSINE ; DEACETYLATION REACTION ; INTERMEDIATE STRUCTURE ; THIOACETYL-LYSINE ; SIR2 DEACETYLASES ; STRUCTURAL BASIS ; MECHANISM ; PROTEIN ; PEPTIDES ; INSIGHTS |
| 资助项目 | National Natural Science Foundation of China[21662010] ; Innovation Team of Natural Science Foundation of Department of Education of Guizhou Province[QJHRCTDZ [2015] ; Cooperative Project of Department of Science and Technology of Guizhou Province[QKHLZ[2015] ; Talent Team Project of Department of Science and Technology of Guizhou Province[QKHPTRC[2016] ; State Key Laboratory of Drug Research[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000438467200006 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279649]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | He, Bin |
| 作者单位 | 1.Guizhou Med Univ, Engn Res Ctr Dev & Applicat Ethn Med & TCM, Guizhou Prov Key Lab Pharmaceut, Sch Pharm,Minist Educ,State Key Lab Funct & Appli, Guiyang 550004, Guizhou, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Chun,Wang, Fang,Chen, Xiaoxue,et al. The mimics of N-epsilon-acyl-lysine derived from cysteine as sirtuin inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(14):2375-2378. |
| APA | Wang, Chun.,Wang, Fang.,Chen, Xiaoxue.,Zou, Yefang.,Zhu, Hong.,...&He, Bin.(2018).The mimics of N-epsilon-acyl-lysine derived from cysteine as sirtuin inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(14),2375-2378. |
| MLA | Wang, Chun,et al."The mimics of N-epsilon-acyl-lysine derived from cysteine as sirtuin inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.14(2018):2375-2378. |
入库方式： OAI收割
来源：上海药物研究所
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