PCV - Programme interdiciplinaire en physique et chimie du vivant

Inhibition de la glucosamine-6P synthase humaine dans le traitement des complications du diabète. – GFATINIB

Submission summary

The hexosamine biosynthetic pathway is associated with the side effects of diabetes through its end-product UDPGlcNAc. The rate limiting step of this pathway, i.e. the conversion of fructose-6P into glucosamine-6P, is catalyzed by glucosamine-6P synthase (hGfat). This enzyme is therefore considered as a therapeutic target to treat the vascular complications (nephro- and retinopathy) of diabetes. A specific inhibitor of hGfat has been recently identified in the laboratory of the project leader from a screening of the chemical library of the Gif Institute. The proposed program intends to optimize this compound after identification of its binding site, to identify new molecules using a rational approach based on the knowledge of the enzyme mechanism and to evaluate their in vitro activity. The goal of this research project is then to identify new inhibitors of hGfat which exhibit a biological activity in cellular models (retina or kidney cells) and/or rodent models able to develop diabetes-related vascular complications. The compounds revealing an interesting potential in animals might be further tested in Human. The partnership between experts in drug design, organic chemistry, enzymology, physical chemistry and physiology of metabolic disease should guarantee the success in the discovery of new and potent hGfat inhibitors with a high added-value.

Project coordination

Marie Ange BADET DENISOT (Organisme de recherche)

The author of this summary is the project coordinator, who is responsible for the content of this summary. The ANR declines any responsibility as for its contents.

Partner

Help of the ANR 500,000 euros
Beginning and duration of the scientific project: - 48 Months

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