G protein-coupled receptor antagonists

Details G protein-coupled receptor antagonists G protein-coupled receptor antagonists

C - Chemistry, Metallurgy

07

K

C07K 14/715 (2006.01) A61K 38/19 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2321962

G-protein coupled receptors (GPCR) generally contain seven transmembrane helices. The present invention provides synthetic peptides derived from these transmembrane helices. The peptides inhibit GPCR function by disrupting GPCR structure. In certain embodiments, charged residues are added at one terminus to promote correct orientation of the peptide in the membrane.

Les récepteurs couplés à la protéine G (GPCR) contiennent généralement sept hélices transmembranaires. La présente invention concerne des peptides synthétiques dérivés de ces hélices transmembranaires. Les peptides de la présente invention inhibent la fonction des GPCR en rompant leur structure. Dans certains modes de réalisation, des résidus chargés sont ajoutés à une extrémité dans le but de faciliter l'orientation correcte du peptide dans la membrane.

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