3-O-甲基-N-乙酰-D-葡萄糖胺在体外对N-乙酰葡糖胺激酶和N-乙酰甘露糖胺激酶的抑制作用。
Inhibition of N-acetylglucosamine kinase and N-acetylmannosamine kinase by 3-O-methyl-N-acetyl-D-glucosamine in vitro.
作者信息
Zeitler R, Giannis A, Danneschewski S, Henk E, Henk T, Bauer C, Reutter W, Sandhoff K
机构信息
Institut für Molekularbiologie und Biochemie, Freien Universität Berlin, Federal Republic of Germany.
出版信息
Eur J Biochem. 1992 Mar 15;204(3):1165-8. doi: 10.1111/j.1432-1033.1992.tb16743.x.
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.
在寻找N-乙酰神经氨酸生物合成抑制剂的过程中，研究表明3-O-甲基-N-乙酰葡糖胺在体外对大鼠肝脏的N-乙酰葡糖胺激酶具有竞争性抑制作用，其Ki值为17微摩尔。N-乙酰甘露糖胺激酶受到非竞争性抑制，Ki值为80微摩尔。在人肝癌细胞系（HepG2）中，3-O-甲基-N-乙酰-D-葡糖胺（1毫摩尔）分别使14C-N-乙酰葡糖胺和14C-N-乙酰甘露糖胺掺入细胞糖蛋白的量减少88%和70%。
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