Design and synthesis of heparin mimetics able to inhibit thrombin. Part 1 - Identification of a hexasaccharide sequence able to inhibit thrombin and suitable for 'polymerisation'

被引：23

作者：

Duchaussoy, P

Jaurand, G

Driguez, PA

Lederman, I

Gourvenec, F

Strassel, JM

Sizun, P

Petitou, M

Herbert, JM

机构：

[1] Sanofi Rech, Haemobiol Res Dept, F-31036 Toulouse, France

[2] Sanofi Chim, F-04201 Sisteron, France

[3] Sanofi Rech, Exploratory Res Dept, F-38184 Montpellier, France

来源：

CARBOHYDRATE RESEARCH | 1999年 / 317卷 / 1-4期

关键词：

heparin; heparin mimetics; antithrombin; Factor Xa; thrombin;

D O I：

10.1016/S0008-6215(99)00067-1

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Three hexasaccharides, having from low to very high affinity for antithrombin, were synthesised from disaccharide building block precursors. One of them, methyl(sodium 2,3-di-O-methyl-4-O-sodium sulfonato-alpha-L-idopyranosyluronate)-(1 --> 4)-[(2,3,6-tri-O-sodium sulfonato-alpha-D-glucopyranosyl)-(1 --> 4)-(sodium 2,3-di-O-methyl-alpha-L-idopyranosyluronate)-(1 --> 4)](2)-2,3,6-tri-O-sodium sulfonato-alpha-D-glucopyranoside, obtainable from a single disaccharide building block precursor, constitutes a good starting point for obtaining simple oligosaccharidic heparin mimetics able to inhibit the two coagulation factors thrombin and Factor Xa. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：63 / 84

页数：22

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