Targeting gli proteins in human cancer by small molecules

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/06 (2006.01) A61K 31/415 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2632813

This invention provides compositions, methods and kits for the diagnosis and treatment of cancers expressing a GLI polypeptide, and in particular a GLI1, GLI2 or GLI3 polypeptide. The invention provides small molecule compounds mimicking the transcriptional activation domain of a GLI polypeptide. The small molecule inhibitors of the invention specifically block the activator function of a GLI polypeptide, but not the repressor function of GLI3.

La présente invention concerne des compositions, des méthodes et des trousses pour diagnostiquer et traiter des cancers exprimant un polypeptide GLI, et en particulier un polypeptide GLI1, GLI2 ou GLI3. L'invention concerne des composés à petites molécules imitant le domaine d'activation transcriptionnelle d'un polypeptide GLI. Les inhibiteurs à petites molécules de l'invention bloquent spécifiquement la fonction activatrice d'un polypeptide GLI, mais pas la fonction répressive de GLI3.

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