Generation of “Neoheparin” from E. coli K5 Capsular Polysaccharide

Heparin remains a major drug in prevention of thromboembolic disease. Concerns related to its animal source have prompted search for heparin analogues. The anticoagulant activity of heparin depends on a specific pentasaccharide sequence that binds antithrombin. We report the generation of a product...

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Veröffentlicht in:Journal of medicinal chemistry 2005-01, Vol.48 (2), p.349-352
Hauptverfasser: LINDAHL, Ulf, LI, Jin-ping, KUSCHE-GULLBERG, Marion, SALMIVIRTA, Markku, ALARANTA, Sakari, VEROMAA, Timo, EMEIS, Jef, ROBERTS, Ian, TAYLOR, Clare, ORESTE, Pasqua, ZOPPETTI, Giorgio, NAGGI, Annamaria, TORRI, Giangiacomo, CASU, Benito
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Sprache:eng
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Zusammenfassung:Heparin remains a major drug in prevention of thromboembolic disease. Concerns related to its animal source have prompted search for heparin analogues. The anticoagulant activity of heparin depends on a specific pentasaccharide sequence that binds antithrombin. We report the generation of a product with antithrombin-binding, anticoagulant, and antithrombotic properties similar to those of heparin, through combined chemical and enzymatic modification of a bacterial (E. coli K5) polysaccharide. The process is readily applicable to large-scale production.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm049812m