Method for screening transglutaminase 2 inhibitor or activator

Details Method for screening transglutaminase 2 inhibitor or activator Method for screening transglutaminase 2 inhibitor or activator

C - Chemistry, Metallurgy

12

Q

C12Q 1/48 (2006.01) C12N 9/10 (2006.01) C12Q 1/02 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2519449

Disclosed herein is a method of screening a candidate compound for a TGase 2 inhibitor or activator, based on the finding that polymerization of I--.kappa.B.alpha. is mediated by TGase 2 and that polymerized I- .kappa.B.alpha. does not inhibit NF--.kappa.B, thereby leading to NF-.kappa.B activation. In the method, the level of free or polymerized I-.kappa.B.alpha. or the level of NF-.kappa.B is measured to determine whether the candidate compound is a TGase 2 inhibitor or activator.

Divulgation d'une méthode de sélection préalable d'un composé candidat pour un inhibiteur ou un activateur de la TGase, basée sur la constatation que la polymérisation de I-kappa.B.alpha. est médiée par la TGase 2 et que I-kappa.B.alpha polymérisée n'inhibe pas NF-kappaB, conduisant de la sorte à l'activation de NF-kappaB. Dans cette méthode, la teneur en I-kappa.B.alpha libre ou polymérisée ou celle de NF-kappaB est mesurée pour déterminer si le composé candidat est un inhibiteur ou un activateur de la TGase 2.

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