Method for the identification of modulators of a secretase...

C - Chemistry – Metallurgy – 12 – Q

Patent

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Details

C12Q 1/68 (2006.01) C12Q 1/02 (2006.01) C12Q 1/34 (2006.01) C12Q 1/37 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2482824

The present invention relates to a cellular screening method for the identification of modulators of secretases. Said method comprises contacting suitable host cells with a test substance wherein said suitable host cells comprise: a) a fusion protein comprising a secretory protein, a membrane anchor domain and a secretase cleavage sequence, b) a protein comprising a secretase activity recognising said cleavage sequence of said fusion protein anda) at least one reporter gene under control of a transcriptional activation system wherein said transcriptional activation system is regulated by the release of said secretory protein from said fusion protein by said secretase activity and its subsequent secretion then culturing said cells under suitable conditions such that said reporter gene allowing detection and/or survival of cells is only expressed or repressed in a manner that is dependent on an altered secretase activity due to said test substance.

L'invention concerne un procédé de criblage cellulaire servant à identifier des modulateurs des sécrétases. Ledit procédé consiste à mettre en contact des cellules hôtes appropriées avec une substance test, lesdites cellules hôtes appropriées comprenant : a) une protéine hybride contenant une protéine sécrétoire, un domaine d'ancrage membranaire et une séquence de clivage des sécrétases, b) une protéine présentant une activité de sécrétase reconnaissant ladite séquence de clivage de ladite protéine hybride et c) au mois un gène rapporteur sous contrôle d'un système d'activation transcriptionnelle régulé par la libération de ladite protéine sécrétoire à partir de ladite protéine hybride par ladite activité de sécrétase et sa sécrétion consécutive. Ledit procédé consiste ensuite à mettre en culture lesdites cellules dans des conditions appropriées de sorte que ledit gène rapporteur permettant la détection et/ou la survie de cellules soit uniquement exprimé ou réprimé dans le cas d'une modification de l'activité de sécrétase provoquée par ladite substance test.

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