Choay J
Semin Thromb Hemost. 1985 Apr;11(2):81-5. doi: 10.1055/s-2007-1004362.
We have synthesized the pentasaccharide representing the binding site of heparin to AT III. This pentasaccharide contains a 3-0-sulfate group on one of its glucosamine units. A pentasaccharide analogue lacking this 3-0-sulfate group and two different tetrasaccharides, each being part of the pentasaccharide sequence with AT III affinity, have also been synthesized. The pentasaccharide with high affinity for AT III also shows high antifactor Xa activity and, in vivo, antithrombotic activity. Removal of glucosamine at the nonreducing end maintains partial binding capacity as well as partial antifactor Xa activity.
我们已经合成了代表肝素与抗凝血酶III（AT III）结合位点的五糖。这种五糖在其一个葡糖胺单元上含有一个3-O-硫酸基团。还合成了一种缺乏该3-O-硫酸基团的五糖类似物以及两种不同的四糖，每种四糖都是具有AT III亲和力的五糖序列的一部分。对AT III具有高亲和力的五糖还表现出高抗Xa因子活性，并且在体内具有抗血栓形成活性。去除非还原端的葡糖胺可维持部分结合能力以及部分抗Xa因子活性。
