Compounds and methods for identifying compounds which...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/48 (2006.01) A61K 38/00 (2006.01) C07K 1/00 (2006.01) C08K 3/34 (2006.01) C08K 7/00 (2006.01) C08K 9/04 (2006.01) C12N 9/52 (2006.01) C12Q 1/37 (2006.01)

Patent

CA 2379269

Compounds and methods for designing and identifying compounds which inhibit TFPP-like aspartyl protease enzymes by targeting the aspartic acid residues of the active site or mimicking peptides corresponding to the region surrounding the substrate's cleavage site are provided. Agents identified as inhibitors of TFPP-like aspartyl proteases such as type 4 prepilin peptidases are expected to be useful as anti-bacterial agents and in inhibiting development of drug resistant strains of bacteria.

L'invention concerne des composés et des procédés servant à mettre au point et à identifier des composés qui inhibent des enzymes d'aspartyl protéases du type TFPP, par le ciblage des résidus d'acide aspartique du site actif ou de peptides mimétiques correspondant à la région entourant le site de coupure du substrat. L'invention concerne des agents identifiés comme des inhibiteurs d'aspartyl protéases du type TFPP, telles des prépiline peptidases du type 4, qui sont présumés utiles comme agents antibactériens et pour inhiber le développement de souches de bactéries résistant aux médicaments.

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