Agents for treating human diseases, especially for treating...

C - Chemistry – Metallurgy – 07 – K

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C07K 14/47 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61K 38/17 (2006.01) G01N 33/50 (2006.01) G01N 33/574 (2006.01)

Patent

CA 2388383

The invention relates to agents for treating human diseases which are based on substances that specifically influence the binding of .beta.-catenin on LEF- 1/TCF- transcription factors, APC or conductin/axin. The invention particularly relates to the identification and use of hydrophobic pockets on the molecular surface in the proximity of the essential binding points for the binding partners of .szlig.-catenin with the aim of optimizing these substances. The invention also relates to the use of the substances, preferably for treating tumors such as colonic cancers and melanomas or for regenerating tissue and promoting hair growth.

L'invention concerne des agents servant à traiter des maladies humaines, à base de substances qui influent spécifiquement sur la liaison de la .beta.-caténine avec des facteurs de transcription LEF-1/TCF, APC ou conductine/axine. Elle concerne en particulier l'identification et l'utilisation de poches hydrophobes à la surface de la molécule à proximité des sites de liaison essentiels pour le partenaire de liaison de la .beta.-caténine, dans le but d'optimiser ces substances. L'invention concerne en outre l'utilisation de ces substances, de préférence pour traiter des tumeurs telles que les carcinomes du côlon et les mélanomes, ou régénérer des tissus et favoriser la croissance des cheveux.

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