Hampton L L, Ladenheim E E, Akeson M, Way J M, Weber H C, Sutliff V E, Jensen R T, Wine L J, Arnheiter H, Battey J F
Laboratory of Molecular Biology, National Institute on Deafness and Other Communication Disorders, National Institutes of Health, Rockville, MD 20850, USA.
Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3188-92. doi: 10.1073/pnas.95.6.3188.
The gastrin-releasing peptide receptor (GRP-R) is one of three members of the mammalian bombesin subfamily of seven-transmembrane G protein-coupled receptors that mediate diverse biological responses including secretion, neuromodulation, chemotaxis, and growth. The X chromosome-linked GRP-R gene is expressed widely during embryonic development and predominantly in gastrointestinal, neuronal, and neuroendocrine systems in the adult. Surprisingly, gene-targeted mice lacking a functional GRP-R gene develop and reproduce normally and show no gross phenotypic abnormalities. However, peripheral administration of bombesin at dosages up to 32 nmol/kg to such mice had no effect on the suppression of glucose intake, whereas normal mice showed a dose-dependent suppression of glucose intake. These data suggest that selective agonists for the GRP-R may be useful in inducing satiety.
胃泌素释放肽受体(GRP-R)是哺乳动物铃蟾肽亚家族中七个跨膜G蛋白偶联受体的三个成员之一,介导多种生物学反应,包括分泌、神经调节、趋化性和生长。X染色体连锁的GRP-R基因在胚胎发育过程中广泛表达,在成体中主要表达于胃肠道、神经元和神经内分泌系统。令人惊讶的是,缺乏功能性GRP-R基因的基因敲除小鼠发育和繁殖正常,且未表现出明显的表型异常。然而,给这些小鼠外周注射高达32 nmol/kg剂量的铃蟾肽对葡萄糖摄取的抑制没有影响,而正常小鼠则表现出剂量依赖性的葡萄糖摄取抑制。这些数据表明,GRP-R的选择性激动剂可能有助于诱导饱腹感。