Core fucosylation is one of the most important glycosylation events in the progression of
liver cancer. For this study, we used an easily handled L-
fucose analog, 2-fluoro-L-fucose (2FF), which interferes with the normal synthesis of
GDP-fucose, and verified its potential roles in regulating core fucosylation and cell behavior in the HepG2
liver cancer cell line. Results obtained from
lectin blot and flow cytometry analysis clearly showed that 2FF treatment dramatically inhibited core fucosylation, which was also confirmed via mass spectrometry analysis. Cell proliferation and
integrin-mediated cell migration were significantly suppressed in cells treated with 2FF. We further analyzed cell colony formation in soft
agar and
tumor xenograft efficacy, and found that both were greatly suppressed in the 2FF-treated cells, compared with the control cells. Moreover, the treatment with 2FF decreased the core fucosylation levels of
membrane glycoproteins such as
EGF receptor and
integrin β1, which in turn suppressed downstream signals that included phospho-EGFR, -AKT, -ERK, and -FAK. These results clearly described the roles of 2FF and the importance of core fucosylation in
liver cancer progression, suggesting 2FF shows promise for use in the treatment of
hepatoma.