SBIR Phase I: Development of a High Throughput Glycosyl-Scanning Platform

This Small Business Innovation Research Phase I project highlights a strategy for the development of the first integrated high throughput pipeline to synthesize and evaluate novel sugar-drug conjugates. The core innovation of this proposed phase I study is an enzyme catalyzed one-step glycosylation reaction that also presents a convenient colorimetric readout amenable to HT-screening. While this phase I study is focused upon the generation and evaluation of novel sugar-drug conjugates for anticancer activity, the fundamental glycosylation platform described can be applied to the synthesis any type of glycoconjugate. Thus, the methodology described has the potential to greatly advance our understanding and exploitation of the role of complex carbohydrates in biology, engineering and medicine. The broader/commercial impacts of this research are both immediate and long term. The immediate gain derives from the rapid generation of small molecule glycosides that, as potential drug discovery leads, will advance the field of medicine. The long term impact of the proposed research will stem from the availability of a technology platform for synthesizing complex carbohydrates that can be easily employed by the nonspecialist. With this technology platform, engineers, biologists, and/or physicians will be able to rapidly generate complex carbohydrates to be employed as novel reagents/scaffolds in material science, nanotechnology, engineering, glycobiology and medicine. Thus, successful development of the proposed pipeline described herein is anticipated to transform the role of sugars well beyond the area of therapeutic development.