Helland A C, Hindsgaul O, Palcic M M, Stults C L, Macher B A
Department of Chemistry, University of Alberta, Edmonton, Canada.
Carbohydr Res. 1995 Oct 16;276(1):91-8. doi: 10.1016/0008-6215(95)00165-p.
UDP-D-galactose:beta-D-galactopyranosyl-(1-->4)-2-acetamido-2-deoxy-D- glucose alpha-(1-->3)-D-galactopyranosyltransferase [E.C. 2.4.1.151] transfers D-galactosyl-residues from the sugar nucleotide with retention of configuration. We report here that synthetic methyl 3'-amino-3'-deoxy-N-acetyllactosaminide (9), where the hydroxyl group normally undergoing galactosylation has been replaced by amino group, is an inhibitor for this enzyme with Ki = 104 microM. The mode of inhibition is not competitive, but appears to be specific, since other glycosyltransferases were not affected by 9.
UDP-D-半乳糖：β-D-吡喃半乳糖基-(1→4)-2-乙酰氨基-2-脱氧-D-葡萄糖α-(1→3)-D-吡喃半乳糖基转移酶[E.C. 2.4.1.151]以构型保留的方式从糖核苷酸转移D-半乳糖基残基。我们在此报告，合成的3'-氨基-3'-脱氧-N-乙酰乳糖胺甲基酯(9)，其中通常进行半乳糖基化的羟基已被氨基取代，是该酶的抑制剂，Ki = 104 microM。抑制模式不是竞争性的，但似乎具有特异性，因为其他糖基转移酶不受9的影响。
