Gefitinib ('Iressa', ZD1839), an epidermal growth factor receptor tyrosine kinase inhibitor, up-regulates p27KIP1 and induces G1 arrest in oral squamous cell …

S Shintani, C Li, M Mihara, J Yano, N Terakado… - Oral oncology, 2004 - Elsevier
S Shintani, C Li, M Mihara, J Yano, N Terakado, K Nakashiro, H Hamakawa
Oral oncology, 2004Elsevier
High expression of epidermal growth factor receptor (EGFR) is frequently observed in many
solid tumor types including oral squamous cell carcinomas (OSCC). Recently, the results of
preclinical studies and early clinical trials targeting the EGFR have shown evidence of the
activity. In this study, gefitinib ('Iressa', ZD1839), an EGFR-tyrosine kinase inhibitor, inhibited
cell proliferation and upregulated p27KIP1 in OSCC cells. Growth inhibition was observed in
OSCC xenografts when mice were treated with gefitinib in vivo. A flow cytometric analysis …
High expression of epidermal growth factor receptor (EGFR) is frequently observed in many solid tumor types including oral squamous cell carcinomas (OSCC). Recently, the results of preclinical studies and early clinical trials targeting the EGFR have shown evidence of the activity. In this study, gefitinib (‘Iressa’, ZD1839), an EGFR-tyrosine kinase inhibitor, inhibited cell proliferation and upregulated p27KIP1 in OSCC cells. Growth inhibition was observed in OSCC xenografts when mice were treated with gefitinib in vivo. A flow cytometric analysis demonstrated that treatment with gefitinib induced accumulation in G1 phase, accompanied by a decrease in the percentage of cells in S phase. Apoptosis was not seen in this study. Cell growth was inhibited by an increase of the cell cycle inhibitor p27KIP1 and a decrease of its ubiquitin ligase subunit Skp2.
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