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Enzymatic Synthesis of Heparin

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Abstract

Heparin and low-molecular-weight heparin have been used as anticoagulant drugs for decades. Pharmaceutical grade heparin is derived from mucosal tissues of slaughtered domestic animals. However, heparin can have severe side effects, has a potential risk of contamination and unstable resources. Thus, synthetic heparin that can be manufactured in a controlled environment is desirable. Although traditional chemical synthesis has successfully reduced the structural complexity of heparin, chemical synthesis of the heparin oligosaccharide is tedious and costly. In this review, we summarize recent progress toward the enzymatic synthesis of heparin/heparan sulfate. We will emphasize the efforts to develop novel enzymatic approaches for the synthesis of heparan sulfate mimics from Escherichia coli heparosan and to produce polysaccharide and oligosaccharide end products with high specificity for the biological target. These advancements provide the foundation for the development of heparan sulfate/heparin-based therapeutic agents.

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Acknowledgements

Our research is supported in part by grants from National Institute of Health (AI050050) and from American Heart Association, MidAtlantic (0855424E).

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  1. Division of Medicinal Chemistry and Natural Product, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599, USA

    Renpeng Liu & Jian Liu

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  1. Renpeng Liu
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  2. Jian Liu
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Correspondence to Renpeng Liu .

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  1. Bradford, 16704, U.S.A.

    Om V. Singh

  2. Edgewood Chemical Biological Center, US Army Medical Research, Blackhawk Road 5183, Aberdeen Proving Ground, 21010-5424, U.S.A.

    Steven P. Harvey

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Liu, R., Liu, J. (2010). Enzymatic Synthesis of Heparin. In: Singh, O., Harvey, S. (eds) Sustainable Biotechnology. Springer, Dordrecht. https://doi.org/10.1007/978-90-481-3295-9_14

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