Method for screening of modulators of calcineurin activity

C - Chemistry – Metallurgy – 12 – N

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C12N 15/12 (2006.01) A61K 38/00 (2006.01) C07K 14/47 (2006.01) C12N 9/02 (2006.01) C12N 9/12 (2006.01) C12N 9/16 (2006.01) C12N 15/53 (2006.01) C12N 15/55 (2006.01) C12N 15/62 (2006.01) C12N 15/70 (2006.01) C12N 15/85 (2006.01) C12Q 1/02 (2006.01) G01N 33/50 (2006.01) G01N 33/573 (2006.01)

Patent

CA 2335278

A method for screening of modulators of calcineurin is provided, which uses the interaction between calcineurin and superoxide dismutase. Modulators of calcineurin are potential candidates for drugs, e.g. for immunesuppressive drugs. The forming of a complex comprising calcineurin and superoxide dismutase is monitorable in the presence of potential activators or inhibitors of calcineurin. Complex formation is performed within the cell by the use of appropriate expression vectors or in vitro using isolated proteins. Preferably, complex formation is monitored by fluorescence detection, especially by laser fluctuation correlation spectroscopy.

Cette technique de criblage de l'activité de la calcineurine fait intervenir l'interaction existant entre la calcineurine et la superoxyde-dismutase. Les modulateurs de la calcineurine sont des candidats potentiels pour des médicaments, notamment des médicaments immunodépresseurs. Il est possible de surveiller la constitution d'un complexe comprenant la calcineurine et la superoxyde-dismutase en présence d'activateurs ou d'inhibiteurs potentiels de la calcineurine. On procède à cette constitution de complexe dans la cellule en utilisant des vecteurs d'expression appropriés ou in vitro à l'aide de protéines isolées. On surveille, de préférence, cette constitution de complexe par détection par fluorescence, en particulier par spectroscopie à corrélation de fluctuations laser.

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