Identifying small organic molecule ligands for binding

G - Physics – 01 – N

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G01N 33/53 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2355215

The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules, wherein those methods take advantage of principles of binding avidity. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.

La présente invention se rapporte à de nouvelles méthodes d'identification rapide et sans ambiguïté de petites molécules organiques qui sont des ligands susceptibles de se lier à des molécules biologiques cibles, lesdites méthodes s'appuyant sur certains principes d'avidité de liaison. Les petites molécules organiques ligands identifiées conformément aux méthodes de cette invention peuvent être utilisées, par exemple, en tant que nouveaux composés chefs de file pour le développement de médicaments thérapeutiques, inhibiteurs d'enzymes, composés de marquage, réactifs de diagnostic, réactifs d'affinité pour la purification de protéines et analogues. Les molécules biologiques cibles incluent, par exemple, des polypeptides, des acides nucléiques, des carbohydrates, des nucléoprotéines, des glycoprotéines, des glycolipides et des lipoprotéines.

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