Non-small-cell lung cancer (NSCLC), the most common type of lung cancer, remains the leading cause of cancer death worldwide. Blocking vascular endothelial growth factor (VEGF) signalling is an effective approach to the treatment of NSCLC. Small molecules have been proven to be good resource for discovery of inhibitors of VEGF signalling. DMH4 is a small molecule that we previously developed and demonstrated to have the property of selectively inhibiting VEGF signalling by targeting VEGF receptor 2 (VEGFR2). In this study, we reported that DMH4 can effectively block phosphorylation of VEGFR2 in both H460 and A549 NSCLC cells, which resulted in significant reduction of NSCLC cell viability in a dose-dependent manner, and the growth inhibition (GI50) of DMH4 against H460 and A549 cell lines were 13.27 and 2.75 mm respectively at 24 h. Our further studies demonstrated that DMH4 significantly suppressed migration and invasion of A549 and H460 cells, and induced apoptosis in those cells. Therefore, DMH4 as a small molecular VEGFR2 inhibitor may represent a new valuable drug lead for NSCLC treatment. (C) 2017 Faculty of Health and Social Sciences, University of South Bohemia in Ceske Budejovice. Published by Elsevier Sp. z o.o. All rights reserved.
基金:
National Natural Science Foundation of China [81272444, 81472744]; Western University of Health Sciences
语种:
外文
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中科院(CAS)分区:
出版当年[2019]版:
大类|4 区医学
小类|4 区药学
最新[2025]版:
大类|4 区医学
小类|4 区医学:研究与实验4 区药学
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出版当年[2018]版:
Q4PHARMACOLOGY & PHARMACY
最新[2023]版:
Q3MEDICINE, RESEARCH & EXPERIMENTALQ3PHARMACOLOGY & PHARMACY
第一作者机构:[1]Hebei Univ, Coll Life Sci, Dept Cell Biol, Baoding, Hebei, Peoples R China[2]Western Univ Hlth Sci, Coll Osteopath Med Pacific, Dept Basic Med Sci, Pomona, CA 91766 USA
通讯作者:
通讯机构:[1]Hebei Univ, Coll Life Sci, Dept Cell Biol, Baoding, Hebei, Peoples R China[2]Western Univ Hlth Sci, Coll Osteopath Med Pacific, Dept Basic Med Sci, Pomona, CA 91766 USA[4]Western Univ Hlth Sci, Coll Vet Med, Pomona, CA 91766 USA[*1]Western University of Health Sciences, College of Osteopathic Medicine of the Pacific, Department of Basic Medical Sciences, Pomona, California, USA.[*2]Western University of Health Sciences, College of Veterinary Medicine, Pomona, CA 91766, USA
推荐引用方式(GB/T 7714):
Li Hao,Ha Helen L.,Ding Xiaoxu,et al.DMH4, a VEGFR2 inhibitor, effectively suppresses growth and invasion of lung cancer cells[J].JOURNAL OF APPLIED BIOMEDICINE.2018,16(1):46-50.doi:10.1016/j.jab.2017.10.006.
APA:
Li, Hao,Ha, Helen L.,Ding, Xiaoxu,Bae, Chay,Gazy, Nicky...&Zhong, Li.(2018).DMH4, a VEGFR2 inhibitor, effectively suppresses growth and invasion of lung cancer cells.JOURNAL OF APPLIED BIOMEDICINE,16,(1)
MLA:
Li, Hao,et al."DMH4, a VEGFR2 inhibitor, effectively suppresses growth and invasion of lung cancer cells".JOURNAL OF APPLIED BIOMEDICINE 16..1(2018):46-50