RT Journal Article
SR Electronic
T1 <em>In Vitro</em> Anticancer Activity of PI3K Alpha Selective Inhibitor BYL719 in Head and Neck Cancer
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 175
OP 182
VO 35
IS 1
A1 BHUMSUK KEAM
A1 SOYEON KIM
A1 YONG-OON AHN
A1 TAE MIN KIM
A1 SE-HOON LEE
A1 DONG-WAN KIM
A1 DAE SEOG HEO
YR 2015
UL http://ar.iiarjournals.org/content/35/1/175.abstract
AB 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.