Development of a High-Throughput Assay for Screening of gamma-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila gamma-Secretase
文献类型：期刊论文
| 作者 | Wang, Lie-Feng2; Zhang, Ru2; Xie, Xin1,2
|
| 刊名 | MOLECULES
 |
| 出版日期 | 2009-09 |
| 卷号 | 14期号:9页码:3589-3599 |
| 关键词 | gamma-secretase inhibitor fluorogenic substrate high throughput screening |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules14093589 |
| 文献子类 | Article |
| 英文摘要 | Selective lowering of amyloid-beta levels with small-molecule gamma-secretase inhibitors is a promising therapeutic approach for Alzheimer's disease. In this work, we developed a high throughput assay for screening of gamma-secretase inhibitors with endogenous gamma-secretase and a fluorogenic substrate. The IC50 values of known gamma-secretase inhibitors generated with this method were comparable with reported values obtained by other methods. The assay was optimized and applied to a small-scale screening of 1,280 compounds. The discovery of several new inhibitors warrants further investigation. This assay was also proven to be easily adopted to test compounds for drosophila and mouse gamma-secretase, which could be very useful to assess compounds activity against gamma-secretase from different species before the in vivo test in animal models. |
| WOS关键词 | ALZHEIMERS-DISEASE ; PRESENILIN ; HETERODIMER ; MODULATION ; NICASTRIN ; BRAIN ; STATE |
| 资助项目 | Ministry of Science and Technology of China[2008DFB30150] ; Shanghai Commission of Science and Technology[08410703500] ; Shanghai Commission of Science and Technology[08431910100] ; Shanghai Commission of Science and Technology[09PJ1410000] ; Shanghai Commission of Science and Technology[09DZ2260100] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000270201900035 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279151]  |
| 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 | Xie, Xin |
| 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.Tongji Univ, Sch Life Sci & Technol, Lab Receptor Based Biomed, Shanghai 200092, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Wang, Lie-Feng,Zhang, Ru,Xie, Xin. Development of a High-Throughput Assay for Screening of gamma-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila gamma-Secretase[J]. MOLECULES,2009,14(9):3589-3599. |
| APA | Wang, Lie-Feng,Zhang, Ru,&Xie, Xin.(2009).Development of a High-Throughput Assay for Screening of gamma-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila gamma-Secretase.MOLECULES,14(9),3589-3599. |
| MLA | Wang, Lie-Feng,et al."Development of a High-Throughput Assay for Screening of gamma-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila gamma-Secretase".MOLECULES 14.9(2009):3589-3599. |
入库方式： OAI收割
来源：上海药物研究所
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