Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce A Generation
文献类型：期刊论文
| 作者 | Zhang, Chenlu1; Wang, Xiaoyin1; Cui, Jin2; Li, Xiaohang2; Zhang, Yangming1 ; Wang, Xin2; Gu, Haifeng1; Li, Wei2; Xie, Xin1; Zhao, Jian2
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| 刊名 | CHINESE JOURNAL OF CHEMISTRY
 |
| 出版日期 | 2017-01 |
| 卷号 | 35期号:1页码:103-112 |
| 关键词 | Alzheimer's disease PS1 BACE1 interaction A betulinic acid SAR |
| ISSN号 | 1001-604X |
| DOI | 10.1002/cjoc.201600611 |
| 文献子类 | Article |
| 英文摘要 | The lupane-type triterpenoids are endowed with a wide range of biological activities such as antiviral, anti-inflammatory and anticancer activity. We describe here its potential application in Alzheimer's disease (AD) treatment as an inhibitor of PS1/BACE1 interaction. 3--Akebonoic acid, which emanated from a high throughput screening (HTS), was discovered to interfere with PS1/BACE1 interaction and reduce amyloid -protein (A) production. In view of the limited source, we instead used naturally rich betulinic acid (compound 2) as starting material for lead optimization and a focused library of its derivatives was constructed to gain a better understanding of the structure activity relationship (SAR) of triterpenoid-type inhibitor of PS1/BACE1 interaction. Compound 22 was finally chosen as the most potent PS1/BACE1 interaction inhibitor, which reduced A generation effectively. |
| WOS关键词 | ALZHEIMERS-DISEASE ; BACE1 ; PRESENILIN-1 ; DERIVATIVES |
| 资助项目 | National Natural Science Foundation of China[81573267] ; National Natural Science Foundation of China[91413103] ; National Natural Science Foundation of China[91213303] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5923748 |
| WOS记录号 | WOS:000393979900016 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275737]  |
| 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 |
| 通讯作者 | Zhao, Jian; Pei, Gang; Nan, Fajun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, State Key Lab Cell Biol, Shanghai 200031, Peoples R China; 3.Tongji Univ, Shanghai East Hosp, Sch Med, Translat Med Ctr Stem Cell Therapy, Shanghai 200092, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Chenlu,Wang, Xiaoyin,Cui, Jin,et al. Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce A Generation[J]. CHINESE JOURNAL OF CHEMISTRY,2017,35(1):103-112. |
| APA | Zhang, Chenlu.,Wang, Xiaoyin.,Cui, Jin.,Li, Xiaohang.,Zhang, Yangming.,...&Nan, Fajun.(2017).Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce A Generation.CHINESE JOURNAL OF CHEMISTRY,35(1),103-112. |
| MLA | Zhang, Chenlu,et al."Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce A Generation".CHINESE JOURNAL OF CHEMISTRY 35.1(2017):103-112. |
入库方式： OAI收割
来源：上海药物研究所
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