Biocidal molecules, macromolecular targets and methods of...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/47 (2006.01) A01N 37/46 (2006.01) A01N 63/00 (2006.01) A61K 38/17 (2006.01) A61P 31/04 (2006.01) C12Q 1/18 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2398808

A method for identifying a compound that has a biocidal effect against a selected organism involves screening from among known or unknown peptide or non-peptide molecules, a test molecule that binds selectively to a target sequence of a multi-helical lid of a heat shock protein of the organism. The binding of the test compound inhibits the protein folding activity of the protein. A specific embodiment of such a method is useful for identifying or designing a pharmaceutical or veterinary biocidal or antibiotic compound, preferably a pathogen and/or strain-specific compound. For this purpose, the compound does not bind to a heat shock protein that is homologous to the mammalian subject to be treated with the compound. Screening methods can encompass direct binding or competitive assays. Molecules or compounds identified by these methods are employed as biocides for pharmaceutical, veterinary, pesticide, insecticide and rodenticide uses, among others.

La présente invention concerne un procédé d'identification d'un composé présentant une activité biocide contre un organisme désigné. A cet effet, on recherche systématiquement parmi des molécules peptides et non peptides connues ou inconnues une molécule de test capable de liaison sélective à une séquence cible d'un couvercle de protéine de stress de l'organisme. La liaison du composé de test inhibe chez cette protéine l'activité de repliement de la protéine. L'un des modes de réalisation d'un tel procédé convient à l'identification ou la conception d'un composé biocide ou antibiotique pharmaceutique ou vétérinaire, de préférence d'un composé spécifique d'un pathogène et/ou d'une souche. A cet effet, le composé ne se lie pas à la protéine de choc qui est homologue du sujet mammalien à traiter avec le composé. Les procédés de recherche systématique peuvent comporter des procédures à liaison directe ou d'essais par compétition. Les molécules ou composés identifiés au moyen de ces procédés conviennent comme biocides à vocations notamment pharmaceutiques, vétérinaires, pesticides, insecticides et rodenticides.

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