Human g protein-coupled receptor and modulators thereof for...

C - Chemistry – Metallurgy – 12 – N

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C12N 15/12 (2006.01) A61K 45/00 (2006.01) A61P 9/10 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) G01N 33/74 (2006.01)

Patent

CA 2621144

The present invention relates to methods of using a G protein-coupled receptor (GPCR), for example GPR84, to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-I expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

L'invention porte sur des méthodes d'utilisation du récepteur couplé aux protéines G (GPCR) pour identifier si un composé candidat peut être un modulateur de l'athérogénèse, le GPCR étant humain dans certaines variantes. Les agonistes de l'invention s'avèrent d'utiles agents thérapeutiques de prévention ou de traitement de: l'athérosclérose et des troubles athérosclérotiques, y compris les maladies des artères coronaires, l'infarctus du myocarde, maladies des artères périphériques, et ischémie cérébrale. Les agonistes de l'invention s'avèrent en outre utiles en tant qu'agents thérapeutiques de prévention ou de traitement de troubles liés à l'expression du MCP-1 dont non exclusivement l'arthrite rhumatoïde, la maladie de Crohn et la sclérose en plaques.

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