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• W2028297948 endingPage "957" @default.
• W2028297948 startingPage "953" @default.
• W2028297948 abstract "Elevated expression of fucosylated glycoconjugates and fucosyltransferases (Fuc-Ts) is found in various tumor cells and has been correlated with aspects of tumor progression such as cell adhesion and metastasis. Thus, fucosyltransferase inhibitors are potentially useful as anti-tumor agents. In the present study, three known spirocyclic drimanes (1, 2, and 3) were isolated from the culture broth of the fungus Stachybotrys cylindrospora. Compound 1 (stachybotrydial) exhibits potent inhibitory activity against alpha1,3-fucosyltransferase (Fuc-TV) during screening, while compounds 2 and 3 show no such inhibitory activity. Kinetic analysis indicates that compound 1 is an uncompetitive inhibitor with respect to GDP-fucose and a noncompetitive inhibitor with respect to N-acetyllactosamine with Ki values of 10.7 and 9.7 microM, respectively. In addition, all three compounds also possess inhibitory activity against sialyltransferase (ST) but not against beta1,4-galactosyltransferase. These observations provide novel chemical structure information that will help in the design of novel Fuc-T and ST inhibitors." @default.
• W2028297948 created "2016-06-24" @default.
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• W2028297948 date "2005-06-01" @default.
• W2028297948 modified "2023-09-25" @default.
• W2028297948 title "Stachybotrydial, a potent inhibitor of fucosyltransferase and sialyltransferase" @default.
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• W2028297948 doi "https://doi.org/10.1016/j.bbrc.2005.03.232" @default.
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