Carbohydrate-based therapeutic

Vital to the discovery of new carbohydrate based therapeutic agents is an understanding of the critical role that carbohydrates play in the biological activity of medicinally active natural products. It has long been recognized that... 

In this new era of functional genomics, it is anticipated that more tools will be developed to facilitate discovery in glycobiology and that carbohydrate-based therapeutic breakthroughs will be realized. 

The pharmaceutical impact of carbohydrate-based therapeutics can also be seen in the agents now under evaluation in pre-clini-cal and clinical development. For example, synthetic carbohydrate chains, modeled on tumor cell antigens but modified to stimulate an immune response, are being used to develop novel cancer vaccines. 

Oseltamivir (9) is a prodrug that is converted to free acid in the body, and the resulting molecule retains the carboxylate bonds found in sialic acid (7).It also makes use of a hydrophobic group that apparently binds better than a glycerol of sialic acid (7) that it replaces. The antibiotics zanamivir (8)and oseltamivir (9) are outstanding examples of new carbohydrate-based therapeutics. 

The reasons why drotrecogin alfa is included as a carbohydrate-based therapeutic is not only because it is a glycoprotein but also because to be fully active the core protein C must be glycosylated by the addition of four Asn-linked oligosaccharides. Other post-translational modifications required for activity include the addition of nine y-carboxy-ghita-... 

In the past decade there has been significant progress in development of carbohydrate-based therapeutics. Also, new methods for the large-scale production of carbohydrates and their analogs are allowing the thorough evaluation of their safety and efficacy in human trials. 

Cancer. The development of carbohydrate-based vaccines designed to activate T-cells targeting of cancer cells has been pursued for some time. The goal of a cancer vaccine is to make the host immune system responsive to antigens characteristic of cancer cells. Several carbohydrate-based therapeutics that have now reached clinical trials seek to estab-... 

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