Benzophenone-linked crf and crf-like peptides for covalent...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/575 (2006.01) C07K 1/14 (2006.01) C07K 14/46 (2006.01) C07K 14/47 (2006.01) G01N 33/53 (2006.01) G01N 33/566 (2006.01) G01N 33/58 (2006.01) G01N 33/68 (2006.01) G01N 33/74 (2006.01)

Patent

CA 2457853

The present invention relates to a ligand of the Corticotropin-Releasing Factor (CRF)-binding protein (CRFBP) selected from the group consisting of CRF, Urocortin (Ucn), and Urotensin, said ligand comprising a covalently linked benzophenone moiety. Further, the present invention relates to a process for the purification of a CRFBP which comprises reacting said CRFBP with the ligand of the invention, performing photoaffinity labeling, and purifying the resultant photoreaction products by HPLC. The present invention also relates to the use of the ligand of the invention for detecting CRFBP and for identifying the binding site within CRFBP. The present invention also relates to a method for identifying an inhibitor of the binding of ARF to CRFBP.

L'invention concerne un ligand de la protéine (CRFBP) de liaison à la corticolibérine (CRF) choisi dans le groupe constitué de CRF, urocortine (Ucn) et urotensine, ce ligand comprenant une fraction benzophénone liée par covalence. L'invention concerne également un procédé de purification d'une CRFBP qui consiste à faire réagir ladite CRFBP avec le ligand selon l'invention, à effectuer un marquage par photoaffinité et à purifier par HPLC les produits de photoréaction résultants. L'invention concerne en outre l'utilisation du ligand selon l'invention afin de détecter la CRFBP et d'identifier le site de liaison dans la CRFBP. L'invention concerne enfin une méthode permettant d'identifier un inhibiteur de la liaison de ARF avec CRFBP.

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