Background: We have recently shown a frequent upregulation of Src-family
kinases (SFK) in head and neck squamous cell carcinoma (HNSCC). Here we
tested, if SFK targeting is effective especially in HNSCC cells with upregulated
SFK signaling.
Methods: The impact of SFK inhibitors SU6656, PP2 and dasatinib on three
HNSCC cell lines with different SFK activity levels was analyzed using proliferation
and colony formation assays, Western blot and functional kinomics.
Results: Proliferation was blocked by all inhibitors in a micro-molar range.
With respect to cell kill, dasatinib was most effective, while SU6656 showed
moderate and PP2 minor effects. Cellular signaling was affected differently, with
PP2 having no effect on SFK signaling while dasatinib probably has non-SFK
specific effects. Only SU6656 showed clear SFK specific effects on signaling.
Conclusion: The results demonstrate potential benefit of SFK inhibition in HNSCC
but they also highlight challenges due to non-specificities of the different drugs.

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