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

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

Abstract

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.

Citation

Lindahl, U., Li, J.-P., Kusche-Gullberg, M., Salmivirta, M., Alaranta, S., Veromaa, T., Emeis, J., Roberts, I., Taylor, C., Oreste, P., Zoppetti, G., Naggi, A., Torri, G., & Casu, B. (2005). Generation of “Neoheparin” from E. coli K5 Capsular Polysaccharide. Journal of Medicinal Chemistry, 48(2), 349-352. https://doi.org/10.1021/jm049812m

• Journal Article Type: Article
• Online Publication Date: Dec 31, 2004
• Publication Date: Jan 27, 2005
• Deposit Date: Jul 27, 2016
• Journal: Journal of Medicinal Chemistry
• Print ISSN: 0022-2623
• Electronic ISSN: 1520-4804
• Publisher: American Chemical Society
• Peer Reviewed: Peer Reviewed
• Volume: 48
• Issue: 2
• Pages: 349-352
• DOI: https://doi.org/10.1021/jm049812m
• Keywords: Thromboembolic disease, heparin
• Public URL: http://researchrepository.napier.ac.uk/Output/318128