Chemoenzymatic synthesis of heparan sulfate and heparin

Abstract

Heparan sulfate (HS) is a highly sulfated polysaccharide that plays essential physiological and pathophysiological functions. The biosynthesis of HS involves a series of specialised sulfotransferases, an epimerase and glycosyl transferases. The availability of these enzymes offers a promising method to prepare HS polysaccharides and structurally defined oligosaccharides. Given the fact that chemical synthesis of large HS oligosaccharides is extremely difficult, preparation of HS using a chemoenzymatic approach has gained momentum. This review article summarises recent progress on the development of a chemoenzymatic approach to prepare HS and HS oligosaccharides.

Keywords::

• heparin
• heparan sulfate
• sulfotransferase
• chemoenzymatic synthesis

Declaration of interest: This work is supported in part by National Institutes of Health Grants AI50050, HL094463, HL096972 and AI074775. Timothy O’Leary is partly supported by a National Institutes of Health-funded program for initiative for maximizing student diversity (5R25GM055336). The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the article.