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IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities
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
2013-10-28
DOI10.1016/j.canlet.2013.07.005
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
WOS记录号WOS:000325587500010
引用统计
被引频次:15[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64526
专题北京大学药学院
北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学药学院_化学生物学系
北京大学药学院_药学院
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
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GB/T 7714
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.
APA Li, Ying-Bo.,Wang, Zhong-Qing.,Yan, Xu.,Chen, Mei-Wan.,Bao, Jiao-Lin.,...&Li, Run-Tao.(2013).IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities.CANCER LETTERS,340(1),88-96.
MLA Li, Ying-Bo,et al."IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities".CANCER LETTERS 340.1(2013):88-96.
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