Generation of "Neoheparin" from E coli K5 capsular polysaccharide

被引:97
作者
Lindahl, U
Li, JP
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
机构
[1] Univ Manchester, Sch Biol Sci, Manchester M13 9PT, Lancs, England
[2] Inalco, Ric Sperimentali Montale, I-50137 Montale, Italy
[3] G Ronzoni Inst Chem & Biochem Res, Milan, Italy
[4] TNO, Prevent & Hlth, Div Vasc & Connect Tissue Res, NL-2333 CK Leiden, Netherlands
[5] BioTie Therapies Corp, FIN-20520 Turku, Finland
[6] Uppsala Univ, Dept Med Biochem & Microbiol, SE-75123 Uppsala, Sweden
关键词
D O I
10.1021/jm049812m
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:349 / 352
页数:4
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