@article {KEAM175, author = {BHUMSUK KEAM and SOYEON KIM and YONG-OON AHN and TAE MIN KIM and SE-HOON LEE and DONG-WAN KIM and DAE SEOG HEO}, title = {In Vitro Anticancer Activity of PI3K Alpha Selective Inhibitor BYL719 in Head and Neck Cancer}, volume = {35}, number = {1}, pages = {175--182}, year = {2015}, publisher = {International Institute of Anticancer Research}, 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) p110α, 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 G0/G1 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}, URL = {https://ar.iiarjournals.org/content/35/1/175}, eprint = {https://ar.iiarjournals.org/content/35/1/175.full.pdf}, journal = {Anticancer Research} }