Oxadiazoline and thiadiazoline ligands for modulating the...

C - Chemistry – Metallurgy – 12 – N

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C12N 15/63 (2006.01) A61K 31/4245 (2006.01) C07D 271/06 (2006.01) C07D 271/07 (2006.01) C07D 413/12 (2006.01) C07D 498/10 (2006.01) C12P 21/02 (2006.01)

Patent

CA 2516270

The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

L'invention concerne des ligands non stéroïdes pour une utilisation dans un système d'expression de gène inductible à base de récepteur nucléaire, et un procédé de modulation d'expression de gène exogène dans lequel un complexe récepteur d'ecdysone comprenant un domaine de liaison d'ADN, un domaine de liaison de ligand, un domaine de transactivation et un ligand est mis en contact avec une construction d'ADN comprenant le gène exogène et un élément de réponse. Ce gène est sous le contrôle de l'élément de réponse et la liaison du domaine de liaison d'ADN à l'élément de réponse en présence du ligand entraîne l'activation ou la suppression du gène.

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