Identification of kinase inhibitors

Details Identification of kinase inhibitors Identification of kinase inhibitors

G - Physics

01

N

G01N 33/573 (2006.01) C12Q 1/48 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2478981

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 a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.

L'invention concerne l'identification d'inhibiteurs de la protéine kinase, qui se lient de préférence à la conformation inactive d'une protéine kinase cible. Ces inhibiteurs sont identifiés par blocage de la protéine kinase cible dans une conformation inactive, et par utilisation d'une approche de liaison covalente pour identifier des inhibiteurs ciblant de préférence la conformation inactive.

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