title: Growth hormone secretagogue receptor antagonists.
abstract: The patent claims peptidic/nonpeptidic inhibitors of the ghrelin receptor, the growth hormone secretagogue receptor (GHSR) 1A. Among these compounds, it was disclosed that the addition in some compounds of a GlyMetAla tripeptide at the N-terminus of the ghrelin peptide agonists converts them into ghrelin receptor antagonists. One of these peptides, among the few that have been studied in vivo, was shown to be able to reduce food intake and body weight gain in rats.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Modena e R.E, Via Campi 183 41100 Modena, Italy. luca.costantino@unimore.it
authors.forename: Luca
authors.initials: L
authors.lastname: Costantino
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004435:Eating / Q000187:drug effects; D005260:Female; D057809:HEK293 Cells; D006727:Hormone Antagonists / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D054440:Receptors, Ghrelin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection; D015430:Weight Gain / Q000187:drug effects
chemical_list: D019440:Anti-Obesity Agents; C571124:Ghsr1a protein, rat; D006727:Hormone Antagonists; D010455:Peptides; D054440:Receptors, Ghrelin