New synthetic heparin mimetics able to inhibit thrombin and factor Xa

Synthetic pentadeca-, heptadeca- and nonadecasaccharides, comprising an antithrombin III (AT III) binding pentasaccharide prolonged at the non-reducing end by a thrombin binding domain have been obtained. The pentadecasaccharide is the shortest oligosaccharide able to catalyse thrombin inhibition by...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-04, Vol.9 (8), p.1155-1160
Main Authors: Petitou, Maurice, Duchaussoy, Philippe, Driguez, Pierre-A., Hérault, Jean-P., Lormeau, Jean-C., Herbert, Jean-M.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Carbohydrate Sequence
Factor Xa Inhibitors
Heparin - analogs & derivatives
Heparin - chemical synthesis
Heparin - pharmacokinetics
Medical sciences
Models, Chemical
Molecular Sequence Data
Pharmacology. Drug treatments
Thrombin - antagonists & inhibitors
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Summary:Synthetic pentadeca-, heptadeca- and nonadecasaccharides, comprising an antithrombin III (AT III) binding pentasaccharide prolonged at the non-reducing end by a thrombin binding domain have been obtained. The pentadecasaccharide is the shortest oligosaccharide able to catalyse thrombin inhibition by AT III. The nonadecasaccharide is a more potent thrombin inhibitor than standard heparin. The pentadecasaccharide (n = 5) is the shortest oligosaccharide able to inhibit thrombin in the presence of AT III. The nonadecasaccharide (n = 7) is a more potent thrombin inhibitor than standard heparin.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00155-9