PEPTIDE ANTAGONISTS DERIVED FROM THE TRANSMEMBRANE DOMAINS OF G PROTEIN-COUPLED RECEPTORS

摘要

This invention relates to peptides and peptidomimetic compounds that act asantagonists 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) todesign novel peptides and peptidiomimetic compounds that antagonize theactivity of the same or closely related GPCRs from which they are derived. Alead peptide which may also be a preferred peptide antagonist for the human.beta.2-adrenergic receptor is NH2-GIIMGTFTLCWLPFFIVNIVH-COOH.