Expression and purification of the catalytic domain of human vascular endothelial growth factor receptor 2 for inhibitor screening
文献类型：期刊论文
| 作者 | Zhong, L; Guo, XN; Zhang, XH; Wu, ZX; Luo, XM; Jiang, HL; Lin, LP; Zhang, XW; Ding, J |
| 刊名 | Biochimica et biophysica acta-general subjects
 |
| 出版日期 | 2005-04-15 |
| 卷号 | 1722期号:3页码:254-261 |
| 关键词 | Kdr Bac-to-bac Angiogenesis inhibitor Tki-31 |
| ISSN号 | 0304-4165 |
| DOI | 10.1016/j.bbagen.2004.12.015 |
| 通讯作者 | Ding, j() |
| 英文摘要 | Vascular endothelial growth factor (vegf), an endothelial cell-specific mitogen, can act in tumor-induced angiogenesis by binding to specific receptors on the surface of endothelial cells. one such receptor, vegfr-2/kdr, plays a key role in vegf-induced angiogenesis. here, we expressed the catalytic domain of vegfr-2 as a soluble active kinase using bac-to-bac expression system, and investigated correlations between vegfr-2 activity and enzyme concentration, atp concentration, substrate concentration and divalent cation type. we used these data to establish a convenient, effective and non-radioactive elisa screening technique for the identification and evaluation of potential inhibitors for vegfr-2 kinase. we screened 200 rtk target-based compounds and identified one (tki-31) that potently inhibited vegfr-2 kinase activity (ic50 = 0.596 mu m). treatment of nih3t3/kdr cells with tki-31 blocked vegf-induced phosphorylation of kdr in a dose-dependent manner. moreover, tki-31 dose-dependently suppressed huvec tube formation. thus, we herein report a novel, efficient method for identifying vegfr-2 kinase inhibitors and introduce one, tki-31, that may prove to be a useful new angiogenesis inhibitor. (c) 2004 elsevier b.v. all rights reserved. |
| WOS关键词 | TYROSINE KINASE DOMAIN ; INSULIN-RECEPTOR ; IN-VIVO ; ANGIOGENESIS ; IDENTIFICATION ; MECHANISM ; FLK-1 ; FLT-1 ; MICE |
| WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
| WOS类目 | Biochemistry & Molecular Biology ; Biophysics |
| 语种 | 英语 |
| WOS记录号 | WOS:000227910800003 |
| 出版者 | ELSEVIER SCIENCE BV |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2377640 |
| 专题 | 中国科学院大学 |
| 通讯作者 | Ding, J |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res,Div Anti Tumor Pharmacol, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Grad Sch, Beijing, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhong, L,Guo, XN,Zhang, XH,et al. Expression and purification of the catalytic domain of human vascular endothelial growth factor receptor 2 for inhibitor screening[J]. Biochimica et biophysica acta-general subjects,2005,1722(3):254-261. |
| APA | Zhong, L.,Guo, XN.,Zhang, XH.,Wu, ZX.,Luo, XM.,...&Ding, J.(2005).Expression and purification of the catalytic domain of human vascular endothelial growth factor receptor 2 for inhibitor screening.Biochimica et biophysica acta-general subjects,1722(3),254-261. |
| MLA | Zhong, L,et al."Expression and purification of the catalytic domain of human vascular endothelial growth factor receptor 2 for inhibitor screening".Biochimica et biophysica acta-general subjects 1722.3(2005):254-261. |
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来源：中国科学院大学
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