Section of Gastroenterology, Boston University School of Medicine, Boston, Massachusetts, USA.
Curr Opin Endocrinol Diabetes Obes. 2011 Feb;18(1):68-74. doi: 10.1097/MED.0b013e328340ff93.
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.
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.
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.
本文将重点介绍近年来对哺乳动物蛙皮素受体在疾病状态下相关病理生理作用的理解的最新进展,以及对蛙皮素受体药理学的新认识。
关于蛙皮素样肽和哺乳动物蛙皮素受体功能的研究表明,它们对广泛的生理和病理生理状态具有重要的生物学影响。体外和体内的药理学实验以及胃泌素释放肽受体(GRP-R/BB2)和神经介素 B 受体(NMB-R/BB1)的遗传啮齿动物模型的利用进一步阐明了它们在记忆和恐惧行为、抑制肿瘤细胞生长、介导瘙痒和男性生殖行为信号中的作用。所有三种哺乳动物蛙皮素受体都被证明在调节能量平衡方面具有一定的作用。已经完成了对孤儿蛙皮素受体亚型-3(BRS-3/BB3)的选择性高亲和力激动剂和拮抗剂的新合成,这将有助于使用动物模型系统进行进一步的研究。
哺乳动物蛙皮素受体参与能量稳态的调节,可能成为肥胖和某些饮食失调症药物治疗的有吸引力的靶点。对蛙皮素样肽及其各自受体相互作用的新的药理学认识有助于未来治疗和成像上皮细胞来源的肿瘤。