Constitutively desensitized g protein-coupled receptors

Details Constitutively desensitized g protein-coupled receptors Constitutively desensitized g protein-coupled receptors

C - Chemistry, Metallurgy

12

N

C12N 15/12 (2006.01) A01K 67/027 (2006.01) A61K 31/41 (2006.01) A61K 31/417 (2006.01) A61K 31/64 (2006.01) A61K 31/7088 (2006.01) A61K 45/00 (2006.01) C07K 14/705 (2006.01) C07K 14/72 (2006.01) C07K 16/28 (2006.01) C12N 5/10 (2006.01) C12N 15/09 (2006.01) C12N 15/63 (2006.01) C12Q 1/68 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2435047

The present invention relates to modified G-protein coupled receptors (GPCRs). The modified GPCRs of the present invention include GPCRs that have been modified to have altered DRY motifs such that the modified GPCRs are constitutively desensitized. As such, the modified GPCRs of the present invention preferably localize to endocytic vesicles or endosomes in an agonist- independent manner. The invention also relates to methods of screening compounds and sample solutions for GPCR activity using the modified GPCRs.

La présente invention concerne des récepteurs couplés aux protéines G (GPCRs) modifiés. Ces GPCR modifiés comprennent des GPCR qui ont été modifiés pour présenter des motifs DRY modifiés, de telle sorte que les GPCR modifiés sont constitutivement désensibilisés. Ainsi, les GPCR modifiés susmentionnés sont localisés dans des vésicules endocytiques ou dans des endosomes de manière indépendamment des agonistes. La présente invention concerne également des procédés permettant de cribler des composés et des solutions de dosage pour rechercher l'activité des GPCR à l'aide des GPCR modifiés.

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