Assays for the identification of compounds that modulate...

G - Physics – 01 – N

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G01N 33/50 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2683816

This invention demonstrates that KRC molecules have multiple important functions as modulating agents in regulating a wide variety of cellular processes including bone formation and mineralization. TGF-.beta. signaling in osteoblasts promotes the formation of a multimeric complex between KRC, Runx2, Smad3, and the E3 ubiquitin ligase, WWPl which inhibits Runx2 function due to the ability of WWPl to promote Runx2 polyubiquitination and proteasome-dependent degradation. Furthermore, KRC and WWPl form a complex with RSK2 which inhibits RS K2 function due to the ability of WWPl to promote RSK2 ubiquitination. Methods for identifying modulators of KRC activity are provided. Methods for modulating an immune response, bone formation and mineralization and KRC-associated disorders using agents that modulate KRC expression and/or activity are also provided.

La présente invention démontre que les molécules KRC ont de multiples fonctions importantes à titre d'agents de modulation pour réguler une grande variété de processus cellulaires comprenant la formation et la minéralisation osseuse. La signalisation TGF-.beta. dans les ostéoblastes favorise la formation d'un complexe multimère entre KRC, Runx2, Smad3, et l'ubiquitine ligase E3, WWPl qui inhibe la fonction Runx2 grâce à son aptitude à promouvoir la polyubiquitination de Runx2 et la dégradation dépendante du protéosome. De plus, KRC et WWPl forment un complexe avec RSK2 qui inhibe la fonction RS K2 grâce à la capacité de WWPl à promouvoir l'ubiquitination de RSK2. Des procédés permettant d'identifier des modulateurs de l'activité KRC sont proposés. Des procédés permettant de moduler une réponse immunitaire, la formation et la minéralisation osseuse et les troubles associés à KRC au moyen d'agents qui modulent l'expression et/ou l'activité KRC sont également proposés.

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