Methods for regulating the kinase domain of ephb2

Details Methods for regulating the kinase domain of ephb2 Methods for regulating the kinase domain of ephb2

C - Chemistry, Metallurgy

07

K

C07K 14/705 (2006.01) A61K 31/70 (2006.01) A61K 38/17 (2006.01) A61K 45/00 (2006.01) C07K 14/715 (2006.01) C12N 9/12 (2006.01) C12N 15/09 (2006.01) C12Q 1/48 (2006.01) G06F 19/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2437194

The present invention relates to binding pockets of receptor tyrosine kinases (RTKs). The binding pockets may regulate the kinase domain of the receptor tyrosine kinases. In particular, the invention relates to a crystal comprising a binding pocket of a receptor tyrosine kinase that regulates the kinase domain of the receptor tyrosine kinase EphB2. The crystal may be useful for modeling and/or synthesizing mimetics of a binding pocket or ligands that associate with the binding pocket. Such mimetics or ligands may be capable of acting as modulators of receptor tyrosine kinase receptor activity, and they may be useful for treating, inhibiting, or preventing diseases modulated by such receptors. Methods are also provided for regulating the kinase domain of an RTK by changing a binding pocket of the RTK that regulates the kinase domain from an autoinhibited state to an active state or from an active state to an autoinhibited state.

L'invention concerne des poches de liaison de récepteurs de type tyrosine kinase (RTK). Ces poches de liaison régulent le domaine kinase de ces récepteurs. Cette invention concerne, plus particulièrement, un cristal comprenant une poche de liaison d'un récepteur de type tyrosine kinase qui régule le domaine kinase dudit récepteur. Le cristal est utilisé dans le modelage et/ou la synthèse de mimétiques d'une poche de liaison ou de ligands associés à la poche de liaison. Ces mimétiques ou ligands agissent en tant que modulateurs de l'activité du récepteur de type tyrosine kinase, et sont utiles dans le traitement, l'inhibition, ou la prévention de maladies modulées par ces récepteurs. L'invention porte également sur des procédés de régulation du domaine kinase d'un état auto-inhibé vers un état actif ou d'un état actif vers un état auto-inhibé.

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