A Cell-Based High-Throughput Assay for the Screening of Small-Molecule Inhibitors of p53-MDM2 Interaction
文献类型：期刊论文
| 作者 | Li, Jing ; Zhang, Shuyong; Gao, Linghuan; Chen, Ying; Xie, Xin
|
| 刊名 | JOURNAL OF BIOMOLECULAR SCREENING
 |
| 出版日期 | 2011-04 |
| 卷号 | 16期号:4页码:450-456 |
| 关键词 | p53 MDM2 small-molecule inhibitor protein-protein interaction high-throughput screening |
| ISSN号 | 1087-0571 |
| DOI | 10.1177/1087057111399191 |
| 文献子类 | Article |
| 英文摘要 | The p53 tumor suppressor is a potent transcription factor that regulates cell growth inhibition and apoptosis. The oncoprotein MDM2 suppresses p53 activity by direct inhibition of its transcriptional activity and enhances the degradation of p53 via the ubiquitin-proteosome pathway. Overexpression of MDM2, found in many human tumors, impairs p53-mediated cell death effectively. Inhibition of the p53-MDM2 interaction can stabilize p53 and may offer a novel strategy for cancer therapy. To search for new inhibitors of the p53-MDM2 interaction, the authors developed a cell-based high-throughput assay system based on mammalian two-hybrid technology. They also used a dual-luciferase reporter system to rule out false-positive hits due to the cytotoxic effect of compounds. Using this assay, they screened a library consisting of 3840 compounds and identified one compound that activates p53 pathway and induces growth arrest in tumor cells.( Journal of Biomolecular Screening. 2011; 16: 450-456) |
| WOS关键词 | PROTEIN-PROTEIN INTERACTION ; P53 FUNCTION ; MDM2 ; ACTIVATION ; TRANSACTIVATION ; DATABASE ; CANCER ; DOMAIN ; TUMORS ; RITA |
| 资助项目 | National Natural Sciences Foundation of China[90713047] ; Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2009CB940900] ; Shanghai Commission of Science and Technology[08DZ2291300] ; Shanghai Commission of Science and Technology[09DZ2291200] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Biotechnology & Applied Microbiology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000289199600008 |
| 出版者 | SAGE PUBLICATIONS INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278570]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Xie, Xin |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Stake Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jing,Zhang, Shuyong,Gao, Linghuan,et al. A Cell-Based High-Throughput Assay for the Screening of Small-Molecule Inhibitors of p53-MDM2 Interaction[J]. JOURNAL OF BIOMOLECULAR SCREENING,2011,16(4):450-456. |
| APA | Li, Jing,Zhang, Shuyong,Gao, Linghuan,Chen, Ying,&Xie, Xin.(2011).A Cell-Based High-Throughput Assay for the Screening of Small-Molecule Inhibitors of p53-MDM2 Interaction.JOURNAL OF BIOMOLECULAR SCREENING,16(4),450-456. |
| MLA | Li, Jing,et al."A Cell-Based High-Throughput Assay for the Screening of Small-Molecule Inhibitors of p53-MDM2 Interaction".JOURNAL OF BIOMOLECULAR SCREENING 16.4(2011):450-456. |
入库方式： OAI收割
来源：上海药物研究所
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