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EPSRC Reference: GR/M85876/01
Title: THE SYNTHESIS OF TRANSITION STATE ANALOGUES AS POTENTIAL GLYCOSYLTRANSFERASE INHIBITORS
Principal Investigator: Davis, Professor B
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Department: Chemistry
Organisation: Durham, University of
Scheme: Standard Research (Pre-FEC)
Starts: 28 February 2000 Ends: 27 August 2001 Value (£): 55,517
EPSRC Research Topic Classifications:
Carbohydrate Chemistry
EPSRC Industrial Sector Classifications:
No relevance to Underpinning Sectors
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Summary on Grant Application Form
The specific inhibition of glycosyltransferases provides valuable mechanistic information about the mode of action of these poorly studied enzymes and is a potential therapeutic strategy in the treatment of disease. The structures and syntheses of several tri-component polyhydroxylated nitrogen heterocycles as transition-state analogue inhibitors of the action of rhamnosyltransferases are proposed. Such inhibitors represent potential therapeutic agents for the treatment of tuberculosis (TB). As a consequence of it's block-wise nature, this methodology is highly flexible and therefore is also applicable to the inhibition of fucosyltransferases in an approach to the treatment of inflammatory diseases and for other glycosyltransferases in an approach to the treatment of inflammatory diseases and for other glycosyltransferases that are mediators in the mechanisms of disease.
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