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IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities
Li Y.-B.; Wang Z.-Q.; Yan X.; Chen M.-W.; Bao J.-L.; Wu G.-S.; Ge Z.-M.; Zhou D.-M.; Wang Y.-T.; Li R.-T.
2013
Source PublicationCancer Letters
Volume340Issue:1Pages:88
Abstract

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. © 2013 Elsevier Ireland Ltd.

KeywordAngiogenesis Breast Cancer Egfr Irreversible Tki
DOI10.1016/j.canlet.2013.07.005
URLView the original
Indexed BySCI
Language英语
WOS Research AreaOncology
WOS SubjectOncology
WOS IDWOS:000325587500010
The Source to ArticleScopus
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, 999078, Macau
Recommended Citation
GB/T 7714
Li Y.-B.,Wang Z.-Q.,Yan X.,et al. IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities[J]. Cancer Letters,2013,340(1):88.
APA Li Y.-B..,Wang Z.-Q..,Yan X..,Chen M.-W..,Bao J.-L..,...&Li R.-T..(2013).IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities.Cancer Letters,340(1),88.
MLA Li Y.-B.,et al."IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities".Cancer Letters 340.1(2013):88.
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