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In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer

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Authors
Keam, Bhumsuk; Kim, Soyeon; Ahn, Yong-Oon; Kim, Tae Min; Lee, Se-Hoon; Kim, Dong-Wan; Heo, Dae Seog
Issue Date
2015-01
Citation
Anticancer Research, Vol.35 No.1, pp.175-182
Keywords
Head and neck squamous cell carcinomaPIK3CABYL719dacomitinib
Abstract
Background/Aim: The purpose of the present study was to explore the antiproliferative effect of BYL719, a specific inhibitor for phosphatidylinositol 3-kinase (PI3K) p110 alpha, in human head and neck cancer cell lines, as a single agent or in combination with the irreversible EGFR tyrosine kinase inhibitor, dacomitinib. Materials and Methods: Six head and neck cancer cell lines consisting of two PIK3CA mutant cell lines, SNU-1076 and Detroit562, and four PIK3CA wild-type cell lines, SNU-1066, SNU-1041, FaDu and SCC25, were analyzed. Results: The PIK3CA-mutant cell lines were more sensitive to BYL719 than the PIK3CA wild-type cell lines. Following BYL719 treatment, all PIK3CA wild-type cell lines, except for the SNU-1066 cell line, exhibited higher IC50 values compared to the PIK3CA mutant cell lines. Administration of BYL719 induced-cell cycle G(0)/G(1) arrest and resulted in increased apoptosis in a dose-dependant manner. Furthermore, the administration of BYL719 reduced the level of p-mTOR, p-AKT and p-S6 expression indicating the down-regulation of downstream signaling. Conclusion: BYL719, a PI3K alpha selective blocker, could be a promising factor in the treatment of head and neck cancer either as a single agent or in combination with dacomitinib.
ISSN
0250-7005
URI
https://hdl.handle.net/10371/165346
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College of Medicine/School of Medicine (의과대학/대학원)Cancer Research Institute (암연구소)Journal Papers (저널논문_암연구소)
College of Medicine/School of Medicine (의과대학/대학원)Internal Medicine (내과학전공)Journal Papers (저널논문_내과학전공)
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