Compositions and methods for inhibiting fungal cell wall...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/10 (2006.01) A01N 43/16 (2006.01) A61K 31/70 (2006.01) C12Q 1/48 (2006.01)

Patent

CA 2209663

Disclosed herein are antifungal compositions having an oligosaccharide that includes an N-acetylhexosamine residue linked .beta.(14) to a hexose and a biologically acceptable carrier. The isolation of the fungal enzyme chitin glucan .beta.(14) transferase (CG.beta.(14)T) is disclosed along with methods for using this enzyme in an assay for antifungal agents. CG.beta.(14)T catalyses the formation of a .beta.(14) linkage between the terminal reducing N-acetylglucosamine residue of chitin and the non-reducing glucose residue of .beta.(13) linked glucans. Inhibitors of the enzyme, antifungals including such inhibitors, methods for the prevention and the treatment of fungal infections in animals and plants, and screening methods for identifying antifungals are also disclosed.

Cette invention se rapporte à des compositions antifongiques comportant un oligosaccharide qui contient un résidu de N-acétylhexosamine lié par une liaison .beta.(1?4) à une hexose, ainsi qu'un excipient acceptable sur le plan biologique. L'isolation de l'enzyme fongique chitine-glucane .beta.(1?4) transférase (CG.beta.(1?4)T), ainsi que des procédés pour utiliser cet enzyme dans des tests de dosage pour agents antifongiques sont également décrits. L'enzyme CG.beta.(1?4)T catalyse la formation d'une liaison .beta.(1?4) entre le résidu de N-acétylglucosamine réducteur terminal de chitine et le résidu de glucose non réducteur des glucanes à liaison .beta.(1?3). Des inhibiteurs de cet enzyme, des agent antifongiques contenant ces inhibiteurs, des procédés pour prévenir et traiter les infections fongiques chez les animaux et les plantes ainsi que des procédés de criblage pour identifier des agents antifongiques sont également présentés.

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