title: Biology and pharmacology of bombesin receptor subtype-3.
abstract: OBJECTIVE
  This review summarizes the results of recent studies regarding the biology and pharmacology of novel synthetic agonists and antagonists of the bombesin receptor subtype-3 (BRS-3).
  
  
  RESULTS
  All three mammalian bombesin receptors including gastrin-releasing peptide receptor, the neuromedin B receptor, and the BRS-3 have been shown to regulate energy balance and appetite and satiety. Studies indicate that the orphan BRS-3 is an important regulator of body weight, energy expenditure, and glucose homeostasis. Endogenous bombesin-like peptides bombesin, gastrin-releasing peptide, and neuromedin B receptor do not bind to BRS-3 and the endogenous BRS-3 ligand remains unknown. The novel synthesis of selective, high-affinity BRS-3 agonists and antagonists has recently been accomplished and showed that BRS-3 regulates energy balance independent of other established pathways and glucose-stimulated insulin secretion in the pancreatic islet cells. The availability of new BRS-3 selective agonists and antagonists will facilitate further elucidation of its role in energy homeostasis, and provides a potential approach for the pharmacological treatment of obesity and type 2 diabetes.
  
  
  CONCLUSIONS
  The native ligand of the G protein-coupled BRS-3 has not been identified as of now. However, novel synthesis of small-molecule, high-affinity agonists and antagonists on the BRS-3 was used in the recent studies and demonstrated an important role of BRS-3 in the regulation of energy homeostasis and glucose metabolism.
authors.affiliation: Section of Gastroenterology, Boston University School of Medicine, Boston, Massachusetts, USA.
authors.forename: Ishita D
authors.initials: ID
authors.lastname: Majumdar
authors.forename: Horst C
authors.initials: HC
authors.lastname: Weber
mesh_terms: D000818:Animals; D001067:Appetite Depressants / Q000494:pharmacology*; D001069:Appetite Regulation / Q000187:drug effects; D001786:Blood Glucose; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000378:metabolism; D004734:Energy Metabolism; D019886:Gastrin-Releasing Peptide / Q000494:pharmacology; D006706:Homeostasis; D006801:Humans; D051379:Mice; D018345:Mice, Knockout; D009765:Obesity / Q000188:drug therapy* / Q000378:metabolism; D018004:Receptors, Bombesin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012528:Satiety Response / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D001067:Appetite Depressants; D001786:Blood Glucose; D018004:Receptors, Bombesin; C107120:bombesin receptor subtype 3; D019886:Gastrin-Releasing Peptide