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- W3115231611 abstract "We report the synthesis and evaluation of a series of cell-permeable and N- versus O-selective sialyltransferase inhibitors. Inhibitor design entailed the functionalization of lithocholic acid at C(3) and at the cyclopentane ring side chain. Among the series, FCW34 and FCW66 were shown to inhibit MDA-MB-231 cell migration as effectively as ST3GALIII-gene knockdown did. FCW34 was shown to inhibit tumor growth, reduce angiogenesis, and delay cancer cell metastasis in animal models. Furthermore, FCW34 inhibited vessel development and suppressed angiogenic activity in transgenic zebrafish models. Our results provide clear evidence that FCW34-induced sialyltransferase inhibition reduces cancer cell metastasis by decreasing N-glycan sialylation, thus altering the regulation of talin/integrin/FAK/paxillin and integrin/NFκB signaling pathways." @default.
- W3115231611 created "2021-01-05" @default.
- W3115231611 creator A5004146901 @default.
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- W3115231611 date "2020-12-28" @default.
- W3115231611 modified "2023-10-17" @default.
- W3115231611 title "Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis" @default.
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- W3115231611 doi "https://doi.org/10.1021/acs.jmedchem.0c01477" @default.
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