In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer.
作者： Bhumsuk Keam , Soyeon Kim , Yong-Oon Ahn , Tae Min Kim , Se-Hoon Lee
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摘要: Background/Aim: The purpose of the present study was to explore antiproliferative effect BYL719, a specific inhibitor for phosphatidylinositol 3-kinase (PI3K) p110α, in human head and neck cancer cell lines, as single agent or combination with irreversible EGFR tyrosine kinase inhibitor, dacomitinib. Materials Methods: Six lines consisting two PIK3CA mutant SNU-1076 Detroit562, four wild-type SNU-1066, SNU-1041, FaDu SCC25, were analyzed. Results: PIK3CA-mutant more sensitive BYL719 than lines. Following treatment, all except SNU-1066 line, exhibited higher IC 50 values compared Administration induced cycle G 0 /G 1 arrest resulted increased apoptosis dose-dependant manner. Furthermore, administration reduced level p-mTOR, p-AKT p-S6 expression indicating down-regulation downstream signaling. Conclusion: PI3K alpha selective blocker, could be promising factor treatment either Head squamous carcinoma (HNSCC) is sixth most common type an annual incidence ~600,000 worldwide (1). Despite advances diagnosis
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