A new model for random screening inhibitors of vascular endothelial growth factor receptor 1 kinase
文献类型：期刊论文
| 作者 | Zhuang, SF; Zhou, CH; Qian, J; Qian, Z; Shibuya, M; Ye, QZ |
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2002-02 |
| 卷号 | 23期号:2页码:117-123 |
| 关键词 | protein-tyrosine kinase drug screening growth factor receptors vascular endothelium |
| ISSN号 | 1671-4083 |
| 文献子类 | Article |
| 英文摘要 | AIM: To establish a 96-well plate based kinase assay using a recombinant vascular endothelial growth factor (VEGF) receptor 1 kinase domain protein. METHODS: A human VEGF receptor 1 kinase domain protein was expressed in E coli, and its activity was monitored by its ability of phosphorylating the polyE4Y substrate coated on the walls of 96-well plates with antibody recognition and a colorimetric readout. A random screening of a sample organic compound library was carried out, and the hits were characterized with a transformed cell line stably expressing VEGF receptor 1 protein. RESULTS: An efficient E coli expressions system for human VEGF receptor 1 kinase domain protein was constructed, and the purified recombinant protein was used to establish a practical screening assay for kinase inhibitors in vitro. Two thousand eight hundred organic compounds were, screened, and two disubstituted furans (A1 and A5) with new structure showed inhibition of VEGF receptor 1 kinase. Compound A1 inhibited only, phosphorylation of substrate, while compound A5 inhibited both autophosphorylation and substrate phosphorylation. Both inhibitors affected phosphorylation in the transformed cells. CONCLUSION: The recombinant receptor kinase based assay is simple and effective, in identifying kinase inhibitors. |
| WOS关键词 | TYROSINE KINASE ; FLT-1 |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:1366600 |
| WOS记录号 | WOS:000173710300004 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274388]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Ye, QZ |
| 作者单位 | 1.Univ Tokyo, Inst Med Sci, Dept Genet, Tokyo, Japan 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhuang, SF,Zhou, CH,Qian, J,et al. A new model for random screening inhibitors of vascular endothelial growth factor receptor 1 kinase[J]. ACTA PHARMACOLOGICA SINICA,2002,23(2):117-123. |
| APA | Zhuang, SF,Zhou, CH,Qian, J,Qian, Z,Shibuya, M,&Ye, QZ.(2002).A new model for random screening inhibitors of vascular endothelial growth factor receptor 1 kinase.ACTA PHARMACOLOGICA SINICA,23(2),117-123. |
| MLA | Zhuang, SF,et al."A new model for random screening inhibitors of vascular endothelial growth factor receptor 1 kinase".ACTA PHARMACOLOGICA SINICA 23.2(2002):117-123. |
入库方式： OAI收割
来源：上海药物研究所
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