Ishita D Majumdar1, Horst C Weber. 1. Section of Gastroenterology, Boston University School of Medicine, Boston, Massachusetts, USA.
Abstract
PURPOSE OF REVIEW: This review will highlight recent advances in the understanding of mammalian bombesin receptor-related pathophysiological roles in disease states and new insights into bombesin receptor pharmacology. RECENT FINDINGS: Studies regarding bombesin-like peptides and mammalian bombesin receptor functions have demonstrated 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) and neuromedin B receptor (NMB-R/BB1) further delineated roles in memory and fear behavior, inhibition of tumor cell growth, mediating signals for pruritus and male reproductive behavior. All three mammalian bombesin receptors were shown to possess some role in the regulation of energy balance. Novel synthesis of selective high affinity agonists and antagonists of the orphan bombesin receptor subtype-3 (BRS-3/BB3) has been accomplished and will facilitate further studies using animal model systems. SUMMARY: Mammalian bombesin receptors participate in the regulation of energy homeostasis and may represent an attractive target for pharmacological treatment of obesity and certain eating disorders. Novel pharmacological insights of bombesin-like peptides and the interaction with their respective receptors have been elucidated to aid future treatment and imaging of epithelial cell-derived tumors.
PURPOSE OF REVIEW: This review will highlight recent advances in the understanding of mammalianbombesin receptor-related pathophysiological roles in disease states and new insights into bombesin receptor pharmacology. RECENT FINDINGS: Studies regarding bombesin-like peptides and mammalianbombesin receptor functions have demonstrated 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) and neuromedin B receptor (NMB-R/BB1) further delineated roles in memory and fear behavior, inhibition of tumor cell growth, mediating signals for pruritus and male reproductive behavior. All three mammalianbombesin receptors were shown to possess some role in the regulation of energy balance. Novel synthesis of selective high affinity agonists and antagonists of the orphan bombesin receptor subtype-3 (BRS-3/BB3) has been accomplished and will facilitate further studies using animal model systems. SUMMARY:Mammalianbombesin receptors participate in the regulation of energy homeostasis and may represent an attractive target for pharmacological treatment of obesity and certain eating disorders. Novel pharmacological insights of bombesin-like peptides and the interaction with their respective receptors have been elucidated to aid future treatment and imaging of epithelial cell-derived tumors.
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