AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR
文献类型：期刊论文
| 作者 | Zhou, Yuanfeng1; Chen, Yi1 ; Tong, Linjiang1; Xie, Hua1; Wen, Weiwei1; Zhang, Jie1; Xi, Yong1; Shen, Yanyan1; Geng, Meiyu1; Wang, Yuanyuan2
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| 刊名 | JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
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| 出版日期 | 2012-10 |
| 卷号 | 16期号:10页码:2321-2330 |
| 关键词 | multi-tyrosine kinases inhibitor angiogenesis anti-tumour activity |
| ISSN号 | 1582-1838 |
| DOI | 10.1111/j.1582-4934.2012.01541.x |
| 文献子类 | Article |
| 英文摘要 | Angiogenesis plays an important role in neoplastic transformation and progression as well as in the metastasis process of most human cancers. Herein, we identified AL3810 as a novel and orally bioavailable small molecular inhibitor with potent inhibitory activity against multiple tyrosine kinases involved in the process of angiogenesis. We found that AL3810 substantially inhibited the autophosphorylation of VEGFR2, PDGFR beta and FGFR1 in endothelial cells. Moreover, AL3810 exhibited potent anti-angiogenesis activity, manifested by significant inhibition of microvessel outgrowth of rat arterial ring and chickallantochorion membrane (CAM) in ex vivo angiogenesis models. Daily dosing of AL3810 has shown broad-spectrum anti-tumour activity in human kidney, pancreas, liver cancer xenograft models. Importantly, immunohistochemistry results demonstrated that the anti-tumour activity of AL3810 was closely correlated with its anti-angiogenesis activity, as demonstrated by a decreased microvessel area and reduced microvessel numbers in tumour tissues. The overall pharmacological profiles of AL3810 are superior to sorafenib. The clinical trials of AL3810 will soon be launched in China. |
| WOS关键词 | ENDOTHELIAL-CELLS ; TUMOR ANGIOGENESIS ; VESSEL MATURATION ; IN-VITRO ; PROGRESSION ; RECEPTORS ; MECHANISM |
| 资助项目 | Key New Drug Creation and Manufacturing Program[2009ZX09301-001] ; Key New Drug Creation and Manufacturing Program[2009ZX09102-021] ; National Natural Science Foundation of China[81072666] ; National Natural Science Foundation of China[20972174] ; Science and Technology Commission of Shanghai Municipality Pujiang Talent Program[10PJ1412000] |
| WOS研究方向 | Cell Biology ; Research & Experimental Medicine |
| 语种 | 英语 |
| WOS记录号 | WOS:000309237500008 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277921]  |
| 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 科研与新药推进处 |
| 通讯作者 | Ding, Jian |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 200031, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discover & Design Ctr, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Yuanfeng,Chen, Yi,Tong, Linjiang,et al. AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR[J]. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE,2012,16(10):2321-2330. |
| APA | Zhou, Yuanfeng.,Chen, Yi.,Tong, Linjiang.,Xie, Hua.,Wen, Weiwei.,...&Ding, Jian.(2012).AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR.JOURNAL OF CELLULAR AND MOLECULAR MEDICINE,16(10),2321-2330. |
| MLA | Zhou, Yuanfeng,et al."AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR".JOURNAL OF CELLULAR AND MOLECULAR MEDICINE 16.10(2012):2321-2330. |
入库方式： OAI收割
来源：上海药物研究所
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