期刊
CURRENT OPINION IN ENDOCRINOLOGY DIABETES AND OBESITY
卷 19, 期 1, 页码 3-7出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/MED.0b013e32834ec77d
关键词
bombesin receptor subtype-3; bombesin-like peptides; energy homeostasis; mammalian bombesin receptors; obesity; synthetic BRS-3 agonist; type 2 diabetes mellitus
资金
- NIH [DK46200]
Purpose of review 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). Recent findings 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. Summary 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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据