European Journal of Biochemistry 1992-03-15

Inhibition of N-acetylglucosamine kinase and N-acetylmannosamine kinase by 3-O-methyl-N-acetyl-D-glucosamine in vitro.

R Zeitler, A Giannis, S Danneschewski, E Henk, T Henk, C Bauer, W Reutter, K Sandhoff

Index: Eur. J. Biochem. 204(3) , 1165-8, (1992)

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Abstract

During the search for inhibitors of N-acetylneuraminic acid biosynthesis, it was shown that 3-O-methyl-N-acetylglucosamine competitively inhibits the N-acetylglucosamine kinase of rat liver in vitro with a Ki value of 17 microM. N-Acetylmannosamine kinase is inhibited non-competitively with a Ki value of 80 microM. In a human hepatoma cell line (HepG2), 3-O-methyl-N-acetyl-D-glucosamine (1 mM) inhibits the incorporation of 14C-N-acetylglucosamine and 14C-N-acetylmannosamine into cellular glycoproteins by 88% and 70%, respectively.