Chemoenzymatic synthesis of homogeneous ultralow molecular weight heparins

Yongmei Xu, Sayaka Masuko, Majde Takieddin, Haoming Xu, Renpeng Liu, Juliana Jing, Shaker A. Mousa, Robert J. Linhardt, Jian Liu

Research output: Contribution to journalArticlepeer-review

348 Scopus citations


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.

Original languageEnglish
Pages (from-to)498-501
Number of pages4
Issue number6055
StatePublished - 28 Oct 2011
Externally publishedYes


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