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学科主题: 药学
题名:
IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities
作者: Li, Ying-Bo1; Wang, Zhong-Qing1; Yan, Xu1; Chen, Mei-Wan2; Bao, Jiao-Lin2; Wu, Guo-Sheng2; Ge, Ze-Mei1; Zhou, De-Min1; Wang, Yi-Tao2; Li, Run-Tao1
关键词: Irreversible TKI ; EGFR ; Angiogenesis ; Breast cancer
刊名: CANCER LETTERS
发表日期: 2013-10-28
DOI: 10.1016/j.canlet.2013.07.005
卷: 340, 期:1, 页:88-96
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Oncology
研究领域[WOS]: Oncology
关键词[WOS]: GROWTH-FACTOR RECEPTOR ; TYROSINE KINASE INHIBITOR ; CELL LUNG-CANCER ; HUMAN BREAST-CANCER ; ACQUIRED-RESISTANCE ; T790M MUTATION ; IN-VIVO ; THERAPY ; GEFITINIB ; STRATEGIES
英文摘要:

Accumulating evidence suggested that the irreversible tyrosine kinase inhibitors (TKIs) have potential to override the acquired resistance to target-based therapies. Herein, we reported IC-4 as a novel irreversible TKI for epidermal growth factor receptor (EGFR). IC-4 potentially suppressed proliferation, induced apoptosis and a G2/M cell cycle arrest in breast cancer cells, correlating with inhibition of EGF-induced EGFR activation, but independent of DNA damage. In addition, IC-4 exhibited anti-angiogenetic activities both in vitro and in vivo. It suppressed cell viability and proliferation induced by various growth factors in human umbilical vein endothelial cells (HUVECs). IC-4 also inhibited HUVECs migration and tube formation. In transgenic zebrafish embryo model, IC-4 was shown to suppress formation of intersegmental vessel and development of subintestinal vessels. Taken together, these results demonstrated that IC-4 is a new irreversible EGFR-TKI, exhibiting potent anti-breast cancer and anti-angiogenetic effects. (C) 2013 Elsevier Ireland Ltd. All rights reserved.

语种: 英语
所属项目编号: 21172011 ; 029/2007/A2
项目资助者: National Natural Science Foundation of China ; Macao Science and Technology Development Fund
WOS记录号: WOS:000325587500010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64526
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Taipa 999078, Peoples R China

Recommended Citation:
Li, Ying-Bo,Wang, Zhong-Qing,Yan, Xu,et al. IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities[J]. CANCER LETTERS,2013,340(1):88-96.
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