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Start Over Descriptor "Heparin, Low-Molecular-Weight chemical synthesis" Journal science new york n y

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2 results on '"Heparin, Low-Molecular-Weight chemical synthesis"'

2. Chemoenzymatic synthesis of homogeneous ultralow molecular weight heparins.

Author

Xu Y, Masuko S, Takieddin M, Xu H, Liu R, Jing J, Mousa SA, Linhardt RJ, and Liu J

Subjects
Animals, Anticoagulants chemistry, Anticoagulants pharmacokinetics, Anticoagulants pharmacology, Antithrombins chemistry, Antithrombins metabolism, Binding Sites, Chemical Phenomena, Fondaparinux, Glycosyltransferases metabolism, Heparin, Low-Molecular-Weight chemistry, Heparin, Low-Molecular-Weight pharmacokinetics, Heparin, Low-Molecular-Weight pharmacology, Molecular Structure, Molecular Weight, N-Acetylglucosaminyltransferases metabolism, Oligosaccharides chemistry, Polysaccharides chemistry, Polysaccharides pharmacokinetics, Polysaccharides pharmacology, Rabbits, Racemases and Epimerases metabolism, Spectrometry, Mass, Electrospray Ionization, Substrate Specificity, Sulfotransferases metabolism, Anticoagulants chemical synthesis, Heparin, Low-Molecular-Weight chemical synthesis
Abstract

Ultralow molecular weight (ULMW) heparins are sulfated glycans that are clinically used to treat thrombotic disorders. ULMW heparins range from 1500 to 3000 daltons, corresponding from 5 to 10 saccharide units. The commercial drug Arixtra (fondaparinux sodium) is a structurally homogeneous ULMW heparin pentasaccharide that is synthesized through a lengthy chemical process. Here, we report 10- and 12-step chemoenzymatic syntheses of two structurally homogeneous ULMW heparins (MW = 1778.5 and 1816.5) in 45 and 37% overall yield, respectively, starting from a simple disaccharide. These ULMW heparins display excellent in vitro anticoagulant activity and comparable pharmacokinetic properties to Arixtra, as demonstrated in a rabbit model. The chemoenzymatic approach is scalable and shows promise for a more efficient route to synthesize this important class of medicinal agent.

Published
2011
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