High affinity inhibitors for target validation and uses thereof

Details High affinity inhibitors for target validation and uses thereof High affinity inhibitors for target validation and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) C12N 9/99 (2006.01) C12Q 1/48 (2006.01)

Patent

CA 2369895

This invention provides general methods for discovering mutant inhibitors for any class of enzymes as well as the specific inhibitors so identified. More specifically, this invention provides general methods for discovering specific inhibitors for multi-substrate enzymes. Examples of such multi--substrate enzymes include, but are not limited to, kinases and transferases. The mutant inhibitors identified by the methods of this invention can be used to highly selectively disrupt cell functions such as oncogenic transformation. In one particular example, this invention provides an Src protein kinase inhibitor, pharmaceutical compositions thereof and methods of disrupting transformation in a ceil that expresses the target v-scr comprising contacting the cell with the protein kinase inhibitor.

L'invention concerne des méthodes générales permettant de découvrir des inhibiteurs mutants dans une classe d'enzymes, ainsi que les inhibiteurs spécifiques ainsi identifiés. Cette invention concerne plus particulièrement des méthodes générales permettant de découvrir des inhibiteurs spécifiques d'enzymes multi-substrats, les kinases et les transférases étant parmi les exemples d'enzymes multi-substrats. Les inhibiteurs mutants identifiés grâce aux méthodes de cette invention peuvent être utilisés pour détruire de manière sélective des fonctions cellulaires, comme la transformation oncogène. Dans un exemple précis, cette invention concerne un inhibiteur de la protéine kinase Src, des compositions pharmaceutiques de ce dernier, et des méthodes destinées à détruire la transformation d'une cellule exprimant l'enzyme v-scr cible, ces méthodes consistant notamment à mettre ladite cellule en présence de l'inhibiteur de protéine kinase.

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