Modulators of itch ubiquitinase activity

A - Human Necessities – 61 – K

Patent

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A61K 45/00 (2006.01) A61K 31/713 (2006.01) A61P 17/00 (2006.01) A61P 35/00 (2006.01) G01N 33/573 (2006.01)

Patent

CA 2592172

The present invention relates to the identification of new drug targets for therapy of disorders including cancer. In particular, the present invention relates to inhibition of the E3 ubiquitin ligase, Itch, as a means for treating disorders. Furthermore, the present invention relates to the regulation of p63 and p73 stability in cells. In particular, the invention relates to the modulation of the regulation of p63 and p73 stability in cells through modulation of the expression or activity of Itch. Moreover, the invention relates to the use of Itch as a target for the development of agents capable of modulating p63 or p73 stability and especially agents capable of modulating the interaction of Itch and p63 or p73. Such agents may be useful in therapeutic applications including cancer treatment and modulation of skin differentiation.

La présente invention porte sur l'identification de nouvelles cibles de médicaments utilisées dans le traitement de maladies telles que le cancer. L'invention porte notamment sur l'inhibition de la ligase ubiquitine E3, Itch, comme moyen de traitement des maladies. L'invention porte, en outre, sur la régulation de la stabilité de p63 et p73 dans des cellules. L'invention porte, en particulier, sur la modulation de la régulation de la stabilité de p63 et p73 par modulation de l'expression ou de l'activité de Itch. L'invention porte, en outre, sur l'utilisation de Itch comme cible dans le développement d'agents capables de moduler la stabilité de p63 ou p73, et notamment d'agents capables de moduler l'interaction de Itch et p63 ou p73. Ces agents peuvent être utiles dans des applications thérapeutiques incluant le traitement du cancer et la modulation de la différenciation de la peau.

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