Development of Oligosaccharides in Drug Discovery

GlycoMar is a developing anti-inflammatory therapies based on saccharide molecules from a wide range of sources including marine organisms. Our recent white paper outlines current saccharide- based drugs on the market or in development, information pills and the opportunity for use of oligosaccharides in drug discovery. It is surprising that there are so few saccharide drugs available – or is it?

Why are there so few saccharide-based drugs?

A few of the big reasons:

Analysis is difficult – structural analysis of saccharides is inherently difficult

Synthesis is difficult – synthesis of all but the simplest saccharides is prohibitively complex

Pharmacology is difficult – saccharides exhibit complex mechanisms of action

Delivery is difficult – these are big polar molecules which don’t obey Lipinski rules

 

While advances are being made on all of these fronts, the field is still some way from offering solutions and of course some characteristics (pharmacology & delivery) are inherent to this class of compounds. Despite these challenges saccharides do offer a valuable range of biological activities, which should be the subject of increased drug discovery research. It is encouraging that increasing numbers of oligosaccharides are becoming commercially available for screening purposes. While the majority of these are prepared from natural products it is notable that synthesis of oligosaccharides is also advancing to provide molecules for screening.

Oligosaccharides libraries from synthetic and natural sources offer opportunity for systematic drug discovery research through their application in high throughput screening systems. In order to have utility in such systems these molecules must be prepared to a high degree of purity and size homogeneity – both of which can be challenging when fractionating oligosaccharides from natural polysaccharides. Glycan arrays have been developed and have proven to be useful as a high- throughput screening method for drug discovery. These can be used to study the interaction of large numbers of saccharide structures with target molecules and can be used to identify possible mechanism(s) of action.

So, oligosaccharide based drug discovery is difficult, but is it worth pursuing? In our white paper we describe a range of biological activity that is proving that this is a worthwhile challenge, delivering a growing therapeutic pipeline.