Polypeptides derived from retinoic acid-related orphan...

C - Chemistry – Metallurgy – 12 – N

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Details

C12N 15/16 (2006.01) C07K 14/705 (2006.01) C12N 15/63 (2006.01) C12P 21/02 (2006.01) G01N 33/50 (2006.01) G06F 19/00 (2006.01)

Patent

CA 2446218

The invention relates to polypeptides derived from the retinoic acid-related orphan receptor (ROR) in mammals, characterized in that they are delimited in their N-terminal extremity by an amino-acid located between positions 1 to 209, and in their C-terminal extremity by an amino-acid located between positions 450 to 452 of the rat ROR.szlig., .alpha., or .gamma., or by an amino-acid located at corresponding positions in nuclear receptor ROR of other subtypes than .alpha., .beta. and .gamma., and/or of the other mammals. The invention also relates to the use of these polypeptides, or of the molecular complexes or the crystals containing them, for carrying out: -a process for the screening of a ROR-LBD ligand which is an agonist, or an antagonist of said receptor, - or a process for the analysis of the tridimensional structure of the complexes formed with said polypeptides, molecular complexes or crystals and a particular compound.

L'invention concerne des polypeptides dérivés du récepteur ROR (récepteur orphelin apparenté aux récepteurs de l'acide rétinoïque), du mammifère. Ces polypeptides sont caractérisés en ce qu'ils sont délimités à leur extrémité N-terminale par un acide aminé placé entre les positions 1 et 209, et à leur extrémité C-terminale par un acide aminé placé entre les positions 450 et 452 du ROR.beta., .alpha. ou .gamma. du rat, ou par un acide aminé placé dans des positions correspondantes dans un récepteur nucléaire ROR appartenant à un sous-type autre que .alpha., .beta. ou .gamma., et/ou d'autres mammifères. L'invention concerne également l'utilisation de ces polypeptides ou de complexes moléculaires ou de cristaux de ces polypeptides pour la mise en oeuvre d'un procédé permettant l'identification d'un ligand ROR-LBD qui est un agoniste ou un antagoniste dudit récepteur, ou d'un procédé permettant l'analyse de la structure tridimensionnelle des complexes formés par lesdits polypeptides, complexes moléculaires ou cristaux et un composé particulier.

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