Chemoenzymatic Synthesis of Heparin

Abstract

Chemoenzymatic synthesis is a strategy to produce heparin oligosaccharides with clearly defined structures and properties. Chemical synthesis involving protection and deprotection is combined with enzymatic synthesis. Chemical synthesis is used to construct appropriate acceptor and donor molecules, while enzymatic synthesis is used in extension and modification. Recombinant enzymes are prepared based on heparin's biosynthetic pathway in animals and capsular polysaccharide pathways in bacteria. Chemoenzymatic synthesis relies on a deep understanding of enzyme spec-ificity and the application of modified unnatural chemically synthesized donors and acceptors to perform target-based synthesis of small-to intermediate-sized heparins.