Heparan sulfate activity, biological

Different values for anticoagulant activity have been reported, but these discrepancies may be explained by contamination with higher sulfated homologues. The similarity between these low sulfated heparans and biologically active heparin resides in the same positive rotation, the same D-glucosamine and D-glucuronic acid moieties, the same resistance to hyal-uronidase, and the same susceptibility to an enz)ane extracted from heparin-adapted flavobacteria. 

Whitelock, J. M. and Iozzo, R. V. (2005). Heparan sulfate A complex polymer charged with biological activity. Chem. Rev. 105, 2745-2764. 

Heparinoid polysaccharides such as heparan sulfate and heparin are able to interact with numerous proteins and influence vital biological processes. Heparinoid mimetics were prepared to reduce the structural complexity of heparinoids and to obtain selectivities. This article summarizes the development of heparinoid mimetics of different classes including representative syntheses and biological activities. Largely simplified compounds with regard to structure and synthetic access are described which maintain or exceed the activity of heparinoid polysaccharides. One of the recipes to increase binding or modify pharmacokinetic parameters was the introduction of hydrophobic groups. 

Both pure dextran sulfates and mixed derivatives of dextran containing sulfate groups exhibit a broad spectrum of biological activities. The structural features of so-called mimetics of heparan sulfate are discussed in Sect. 5.2.2.1. The pure dextran sulfates used are almost exclusively commercial products with DS values above 2.0. 

Shriver, Z., Liu, D., and Sasisekharan, R. (2002). Emerging views of heparan sulfate glycosaminoglycan structure/activity relationships modulating dynamic biological functions. Trends Cardiovasc. Med. 12, 71—II. 

Chen J, Avci FY, Munoz EM, McDowell LM, Chen M, Pedersen LC, Zhang L, Linhardt RJ, Liu J. Enzymatic redesigning of biologically active heparan sulfate. J. Biol. Chem. 2005 280 42817-42825. 

Heparin and heparan sulfate are the most intensively studied GAGs as a result of their anticoagulant properties. However, in last 1-2 decades, it has become obvious that heparin and heparan sulfate not only have anticoagulant activities but also exhibit a number of diverse biological functions including ones regulating cell growth and differentiation, inflammatory processes, host defense... 

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