PBA2 exhibits potent anti-tumor activity via suppression of VEGFR2 mediated-cell proliferation and angiogenesis
文献类型：期刊论文
| 作者 | Fang, Xiaona3; Xie, Hua2 ; Luo, Min3; Chen, Zhen3; Wang, Fang3; Li, Qingshan1; Wang, Xiaokun3; Ding, Jian2; Fu, Liwu3
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| 刊名 | BIOCHEMICAL PHARMACOLOGY
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| 出版日期 | 2018-04 |
| 卷号 | 150页码:131-140 |
| 关键词 | Angiogenesis And-tumor activity Multi-tyrosine kinases inhibitor PBA2 VEGFR2 |
| ISSN号 | 0006-2952 |
| DOI | 10.1016/j.bcp.2018.01.051 |
| 文献子类 | Article |
| 英文摘要 | VEGFR2 (vascular endothelial growth factor receptor 2) is the main trigger of VEGF-mediated angiogenic signal and targeting VEGFR2 pathway to inhibit tumor angiogenesis represents a promising strategy for cancer therapy. We elucidated that a novel compound, PBA2 exhibited potent anti-tumor effects both in vitro and in vivo with limited toxicity. ELISA assay revealed that PBA2 had a strong suppressive activity against VEGFR2 related to angiogenesis. Furthermore, PBA2 considerably disrupted tube formation of endothelial cells in vitro and systemic administration of PBA2 exerted decreased tumor angiogenesis in vivo. Functional tests demonstrated that PBA2 concentration-dependently impeded the migration and proliferation of endothelial cells. PBA2 had no effects on the expression level of VEGF both in the detected cancer cells and endothelial cells. VEGFR2 and its downstream Akt and Erk pathways were blocked by PBA2 in a concentration-dependent manner both in vitro and in vivo. Overall, we first demonstrated that PBA2, targeting VEGFR2 related to angiogenesis, presented remarkable antiangiogenic and anti-tumor activities through attenuating VEGFR2 mediated pathway in vitro and in vivo with limited toxicity. These observations posed that PBA2 could be a potential drug candidate for developing antiangiogenic tyrosine kinase inhibitor in cancer therapy. |
| WOS关键词 | SMALL-MOLECULE INHIBITORS ; GROWTH-FACTOR ; IN-VITRO ; CHEMOTHERAPEUTIC-AGENTS ; CANCER ; THERAPY ; IDENTIFICATION ; ACTIVATION ; MECHANISMS ; KINASES |
| 资助项目 | Natural Scientific Foundation of China[81473233] ; Natural Scientific Foundation of Guangdong Province[2016A030312014] ; Science and Technology Planning Project of Guangdong Esophageal Cancer Research Institute[Q201514] ; Science and Technology project of Guangdong Province[2014B050504004] ; Science and Technology project of Guangdong Province[2013B051000046] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000431287100013 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279818]  |
| 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, Jian; Fu, Liwu |
| 作者单位 | 1.Guangzhou Med Univ, Guangzhou Peoples Hosp 1, Dept Hematol, Guangzhou 510180, Guangdong, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Sun Yat Sen Univ, Guangdong Esophageal Canc Inst, Collaborat Innovat Ctr Canc Med, State Key Lab Oncol South China,Canc Ctr, Guangzhou 510060, Guangdong, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Fang, Xiaona,Xie, Hua,Luo, Min,et al. PBA2 exhibits potent anti-tumor activity via suppression of VEGFR2 mediated-cell proliferation and angiogenesis[J]. BIOCHEMICAL PHARMACOLOGY,2018,150:131-140. |
| APA | Fang, Xiaona.,Xie, Hua.,Luo, Min.,Chen, Zhen.,Wang, Fang.,...&Fu, Liwu.(2018).PBA2 exhibits potent anti-tumor activity via suppression of VEGFR2 mediated-cell proliferation and angiogenesis.BIOCHEMICAL PHARMACOLOGY,150,131-140. |
| MLA | Fang, Xiaona,et al."PBA2 exhibits potent anti-tumor activity via suppression of VEGFR2 mediated-cell proliferation and angiogenesis".BIOCHEMICAL PHARMACOLOGY 150(2018):131-140. |
入库方式： OAI收割
来源：上海药物研究所
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