Peptide antagonists derived from the transmembrane domains...

Details Peptide antagonists derived from the transmembrane domains... Peptide antagonists derived from the transmembrane domains...

C - Chemistry, Metallurgy

12

N

C12N 15/12 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/17 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2252369

This invention relates to peptides and peptidomimetic compounds that act as antagonists against G protein-coupled receptors (GPCRs). Novel short peptides, derived from the transmembrane domains of GPCRs, ranging in size from about 15- 20 amino acid residues, can be used as model peptides (peptide-leads) to design novel peptides and peptidiomimetic compounds that antagonize the activity of the same or closely related GPCRs from which they are derived. A lead peptide which may also be a preferred peptide antagonist for the human .beta.2-adrenergic receptor is NH2-GIIMGTFTLCWLPFFIVNIVH-COOH.

L'invention concerne des composés peptidiques et peptidomimétiques qui agissent comme antagonistes contre les récepteurs couplés aux protéines G (GPCR). De nouveaux peptides courts, dérivés des domaines transmembranaires des GPCR, dont la taille se situe entre 15 et 20 restes d'acides aminés, peuvent être utilisés comme peptides modèles (peptides initiateurs) pour concevoir de nouveaux composés peptidiques et peptidiomimétiques qui sont des antagonistes de l'activité de ces derniers ou étroitement liés aux GPCR dont ils sont dérivés. Un peptide initiateur qui peut également être un antagoniste peptidique préféré pour le récepteur .beta.2-adrénergique de l'homme est le NH¿2?-GIIMGTFTLCWLPFFIVNIVH-COOH.

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