Probe for detecting nuclear receptor agonist or antagonist...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/02 (2006.01) A01K 67/027 (2006.01) C07K 14/72 (2006.01) C07K 19/00 (2006.01) C12N 15/09 (2006.01) G01N 21/78 (2006.01) G01N 33/15 (2006.01)

Patent

CA 2601952

A probe for detecting an agonist or an antagonist to a nuclear receptor characterized in that at least a ligand-recognition site containing a ligand- binding domain of the nuclear receptor is ligated to a binding-responsive site containing a peptide chain specifically binding to a coactivator-binding domain in the ligand-binding domain of the nuclear receptor via a flexible linker, and two marker sites, which allow the detection of the approach to each other, are ligated to the respective ends of the fused structure of [ligand-recognition site/linker/binding-responsive site].

Sonde servant A dEtecter un agoniste ou un antagoniste vis-A-vis d'un rEcepteur nuclEaire caractErisEe en ce qu'au moins un site de reconnaissance de ligand contenant un domaine de liaison A un ligand du rEcepteur nuclEaire est ligaturE A un site sensible A la formation de liaison contenant une chaIne de peptides se liant de faÇon spEcifique A un domaine de liaison A un co-activateur prEsent dans le domaine de liaison A un ligand du rEcepteur nuclEaire via un lieur flexible, et deux sites marqueurs, qui permettent la dEtection de l'approche l'un de l'autre, sont ligaturEs aux extrEmitEs respectives de la structure fusionnEe [site de reconnaissance du ligand/lieur/site sensible A la formation de liaison].

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