TKI-31 inhibits angiogenesis by combined suppression signaling pathway of VEGFR2 and PDGFR beta
文献类型：期刊论文
| 作者 | Zhong, L; Guo, XN; Zhang, XH; Sun, QM; Tong, LJ; Wu, ZX; Luo, XM ; Jiang, HL; Nan, FJ; Zhang, XW
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| 刊名 | CANCER BIOLOGY & THERAPY
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| 出版日期 | 2006-03 |
| 卷号 | 5期号:3页码:323-330 |
| 关键词 | tyrosine kinase VEGFR2 PDGFR beta angiogenesis |
| ISSN号 | 1538-4047 |
| DOI | 10.4161/cbt.5.3.2543 |
| 文献子类 | Article |
| 英文摘要 | Tyrosine kinases have been strongly implicated as therapeutic targets that influence the angiogenic process in growing tumors. In this study, we revealed that TKI-31 is a potent broad spectrum tyrosine kinase inhibitor, which inhibits vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFR beta) and also inhibits kinases of other class, such as c-Kit and c-Src on molecular base, but showed no activity against vascular endothelial growth factor receptor 1 (VEGFR1) and epidermal growth factor receptor ( EGFR). TKI-31 inhibits VEGF-induced phosphorylation of VEGFR2 in endothelial cells as well as PDGFBB-induced phosphorylation in fibroblast cells, and leading to the inhibition of down-stream signaling triggered by these receptors such as PI3K/Akt/mTOR, MAPK42/44( ERK) and paxillin. TKI-31 also inhibited VEGF-induced endothelial cells proliferation, migration and their differentiation into capillary-like tube formation. Its anti-angiogenic property was further confirmed by the inhibition of neovascularization on CAM, in vivo. These results collectively highlight the therapeutic potential of this compound for the treatment of solid tumors and other diseases where angiogenesis plays an important role. |
| WOS关键词 | ENDOTHELIAL GROWTH-FACTOR ; TYROSINE KINASE ; TUMOR ANGIOGENESIS ; TUBE FORMATION ; CANCER ; EXPRESSION ; SURVIVAL |
| WOS研究方向 | Oncology |
| 语种 | 英语 |
| WOS记录号 | WOS:000237608800023 |
| 出版者 | LANDES BIOSCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273657]  |
| 专题 | 药理学第一研究室 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 | Ding, J |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol,State Key Lab Drug Res, Shanghai, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhong, L,Guo, XN,Zhang, XH,et al. TKI-31 inhibits angiogenesis by combined suppression signaling pathway of VEGFR2 and PDGFR beta[J]. CANCER BIOLOGY & THERAPY,2006,5(3):323-330. |
| APA | Zhong, L.,Guo, XN.,Zhang, XH.,Sun, QM.,Tong, LJ.,...&Ding, J.(2006).TKI-31 inhibits angiogenesis by combined suppression signaling pathway of VEGFR2 and PDGFR beta.CANCER BIOLOGY & THERAPY,5(3),323-330. |
| MLA | Zhong, L,et al."TKI-31 inhibits angiogenesis by combined suppression signaling pathway of VEGFR2 and PDGFR beta".CANCER BIOLOGY & THERAPY 5.3(2006):323-330. |
入库方式： OAI收割
来源：上海药物研究所
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