Methods for rapidly identifying small organic ligands

G - Physics – 01 – N

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G01N 33/53 (2006.01) C12Q 1/68 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01) G01N 37/00 (2006.01)

Patent

CA 2336183

The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. 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. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.

L'invention concerne de nouvelles techniques qui permettent d'identifier rapidement et sans ambiguïté des ligands constitués de petites molécules, capables de se lier à des molécules cibles biologiques. Les ligands identifiés selon les techniques de la présente invention peuvent être utilisés, par exemple, comme nouveaux composés chefs de file de médicaments, inhibiteurs enzymatiques, composés de marquage, réactifs diagnostiques, réactifs d'affinité pour la purification de protéines, etc. L'invention concerne également de nouvelles techniques qui permettent d'identifier des ligands présentant une forte affinité de liaison pour une molécule cible biologique d'intérêt. Ces techniques consistent à lier deux ou plusieurs ligands constitués de petites molécules organiques, que l'on a préalablement identifiés comme étant capables de se lier à la molécule cible biologique d'intérêt. Les molécules cibles biologiques peuvent être, par exemple, des polypeptides, des acides nucléiques, des glucides, des nucléoprotéines, des glycoprotéines, des glycolipides ou des lipoprotéines.

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