期刊
BIOMEDICINE & PHARMACOTHERAPY
卷 67, 期 5, 页码 351-356出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biopha.2013.03.012
关键词
Icotinib; Squamous cell carcinoma; PDK1, AKT
资金
- National Natural Science Foundation of China [91129728, 81101563]
- Natural Science Foundation of Jiangsu Province [BK2010579]
- Key Personnel of Jiangsu Province [RC2011170]
- National Science & Technology Major Project [2012ZX09304-001]
- National Fundamental Fund of Personnel Training in Biology [J1210026]
- China International Medical Foundation [CIMF-F-H001-037]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
Icotinib is a potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. In this study, we reported that icotinib had the antitumor activity on human squamous cell carcinoma cell line A431 in vitro. Meanwhile, adhesion to fibronectin and expression of integrin alpha 3 and beta 1 were significantly reduced in a dose-dependent manner after the treatment of icotinib. Moreover, icotinib induced cell cycle arrested and affected expression of various cell cycle related proteins in squamous cancer cell line A431, whereas it did not cause apoptosis. Furthermore, icotinib remarkably down-regulated phosphorylation of protein kinase B (AKT) though blocking the interaction between 3-phosphoinositide-dependent protein kinase-1 (PDK1) and AKT in A431 cells. Taken together, it is shown that the small molecular compound, icotinib, has an anti-squamous cell carcinoma activity in vitro and its antitumor mechanism is associated with the blockage of the interaction between PDK1 and AKT. These results provide a novel strategy for anti-squamous cell carcinoma therapy. (C) 2013 Elsevier Masson SAS. All rights reserved.
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