Peptide antagonists derived from the transmembrane domains of g protein-coupled receptors

摘要

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.