Modulators and inhibitors of fibroblast growth factor...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/02 (2006.01) A61K 39/395 (2006.01) C07K 14/71 (2006.01) C07K 16/28 (2006.01) C12N 15/12 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2487557

Isolated fibroblast growth factor receptor (FGFR5) polypeptides and polynucleotides encoding such polypeptides are provided. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to and agonize or antagonize FGFR5 polypeptide function. Specific binding molecules include antibodies, functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5 and, thus, are effective agents suitable for the treatment of diseases such as osteopontin-mediated autoimmune disease, such as systemic lupus erythematosus, bone disorders including osteoporosis and osteopetrosis, and cancers, including cellular carcinomas such as hepatocellular carcinomas.

L'invention concerne des polypeptides du récepteur 5 du facteur de croissance des fibroblastes (FGFR-5) isolés, ainsi que des polynucléotides codant pour ces polypeptides. L'invention concerne également des modulateurs de l'expression des gènes de FGFR-5, ainsi que des molécules qui se fixent de manière spécifique sur le polypeptides de FGFR-5 et qui servent d'agonistes ou d'antagonistes de la fontion polypeptidique de FGFR-5. Les molécules qui se fixent de manière spécifique comprennent des anticorps, des fragments fonctionnels de ces anticorps, ainsi que des scFv et des IgG à chaîne lourde de Camelidae qui se fixent de manière spécifique sur FGFR-5 et modulent l'activité de FGFR-5. Ces molécules constituent ainsi des agents efficaces pouvant être utilisés dans le traitement de diverses pathologies, telles que la maladie auto-immune induite par l'ostéopontine et notamment le lupus érythémateux disséminé, les troubles osseux et notamment l'ostéoporose et l'ostéopétrose, et les cancers, à savoir les carcinomes cellulaires tels que les carcinomes hépatocellulaires.

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