title: Appetite-modifying effects of bombesin receptor subtype-3 agonists.
abstract: Studies on bombesin-like peptides (BLP) and their respective mammalian receptors (Bn-r) have demonstrated a significant biological impact on a broad array of physiological and pathophysiological conditions. Pharmacological experiments in vitro and in vivo as well as utilization of genetic rodent models of the gastrin-releasing peptide receptor (GRP-R/BB2-receptor), neuromedin B receptor (NMB-R/BB1-receptor), and the bombesin receptor subtype-3 (BRS-3/BB3-receptor) further delineated their role in health and disease. All three mammalian bombesin receptors have been shown to possess some role in the regulation of energy balance and appetite and satiety. Compelling experimental evidence has accumulated indicating that the orphan BRS-3 is an important regulator of body weight, energy expenditure, and glucose homeostasis. BRS-3 possesses no high affinity to the endogenous bombesin-like peptides (BLP) bombesin, GRP, and NMB, and its endogenous ligand remains unknown. Recently, the synthesis of novel, selective high-affinity BRS-3 agonists and antagonists has been accomplished and has demonstrated that BRS-3 regulates energy balance independent of other established pathways. Accordingly, 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.
authors.affiliation: Section of Gastroenterology, Boston University School of Medicine, MA, USA.
authors.forename: Ishita Deb
authors.initials: ID
authors.lastname: Majumdar
authors.forename: H Christian
authors.initials: HC
authors.lastname: Weber
mesh_terms: D000818:Animals; D001067:Appetite Depressants / Q000737:chemistry / Q000494:pharmacology*; D001069:Appetite Regulation / Q000187:drug effects*; D004435:Eating / Q000187:drug effects; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009765:Obesity / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology / Q000523:psychology; D018004:Receptors, Bombesin / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D012528:Satiety Response / Q000187:drug effects; D013329:Structure-Activity Relationship; D015431:Weight Loss / Q000187:drug effects
chemical_list: D001067:Appetite Depressants; D018004:Receptors, Bombesin; C107120:bombesin receptor subtype 3