Chemoenzymatic synthesis of the next generation of ultralow molecular weight heparin therapeutics
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Authors
Masuko, S.
Linhardt, Robert J.
Issue Date
2012
Type
Article
Language
ENG
Keywords
Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
Alternative Title
Abstract
Heparin, a sulfated glycosaminoglycan, is a widely used injectable anticoagulant. This polysaccharide is a natural product extracted from porcine intestinal tissue. A specific pentasaccharide sequence is responsible for heparin's high affinity towards anti-thrombin III, which undergoes a conformational change and, as a result, inhibits the blood coagulation Factor Xa, a critical serine protease at the convergence on the intrinsic and extrinsic activation pathway of the coagulation cascade. Due to its structural complexity and heterogeneity, the synthesis of the anti-thrombin III-binding sequence of heparin has been limited to a few approaches. The heparin contamination crisis in 2007 has motivated the development of alternative methods for the efficient preparation of safe heparin products. In this article, we discuss the current methods and recent advances in heparin and low MW heparin syntheses and the recent successful chemoenzymatic preparation of ultralow MW heparins.
Description
Future Medicinal Chemistry, 4, 289–296
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Full Citation
Chemoenzymatic synthesis of the next generation of ultralow molecular weight heparin therapeutics, S. Masuko, R. J. Linhardt, Future Medicinal Chemistry, 4, 289–296, 2012..
Publisher
Future Science