Identification of kinase inhibitors

G - Physics – 01 – N

Patent

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G01N 33/573 (2006.01) C12Q 1/48 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2539064

The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using Tethering to identify inhibitors preferentially targeting the inactive conformation.

L'invention se rapporte à l'identification d'inhibiteurs de protéines kinases qui se lient de manière préférentielle à la conformation inactive d'une protéine kinase cible. Ces inhibiteurs sont identifiés par verrouillage de la protéine kinase cible dans une conformation inactive, et par un ancrage permettant d'identifier les inhibiteurs ciblant de manière préférentielle la conformation inactive.

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