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International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states.
Pharmacological Reviews ( IF 21.1 ) Pub Date : 2007-11-30 , DOI: 10.1124/pr.107.07108
R T Jensen 1 , J F Battey , E R Spindel , R V Benya
Affiliation  

The mammalian bombesin receptor family comprises three G protein-coupled heptahelical receptors: the neuromedin B (NMB) receptor (BB(1)), the gastrin-releasing peptide (GRP) receptor (BB(2)), and the orphan receptor bombesin receptor subtype 3 (BRS-3) (BB(3)). Each receptor is widely distributed, especially in the gastrointestinal (GI) tract and central nervous system (CNS), and the receptors have a large range of effects in both normal physiology and pathophysiological conditions. The mammalian bombesin peptides, GRP and NMB, demonstrate a broad spectrum of pharmacological/biological responses. GRP stimulates smooth muscle contraction and GI motility, release of numerous GI hormones/neurotransmitters, and secretion and/or hormone release from the pancreas, stomach, colon, and numerous endocrine organs and has potent effects on immune cells, potent growth effects on both normal tissues and tumors, potent CNS effects, including regulation of circadian rhythm, thermoregulation; anxiety/fear responses, food intake, and numerous CNS effects on the GI tract as well as the spinal transmission of chronic pruritus. NMB causes contraction of smooth muscle, has growth effects in various tissues, has CNS effects, including effects on feeding and thermoregulation, regulates thyroid-stimulating hormone release, stimulates various CNS neurons, has behavioral effects, and has effects on spinal sensory transmission. GRP, and to a lesser extent NMB, affects growth and/or differentiation of various human tumors, including colon, prostate, lung, and some gynecologic cancers. Knockout studies show that BB(3) has important effects in energy balance, glucose homeostasis, control of body weight, lung development and response to injury, tumor growth, and perhaps GI motility. This review summarizes advances in our understanding of the biology/pharmacology of these receptors, including their classification, structure, pharmacology, physiology, and role in pathophysiological conditions.

中文翻译:

国际药理学联合会。六十八。哺乳动物铃蟾肽受体:正常和疾病状态下的命名、分布、药理学、信号传导和功能。

哺乳动物铃蟾肽受体家族包含三种 G 蛋白偶联七螺旋受体:神经调节蛋白 B (NMB) 受体 (BB(1))、胃泌素释放肽 (GRP) 受体 (BB(2)) 和孤儿受体铃蟾肽受体亚型 3 (BRS-3) (BB(3))。各受体分布广泛,尤其是在胃肠(GI)道和中枢神经系统(CNS)中,受体在正常生理和病理生理条件下都具有广泛的作用。哺乳动物铃蟾肽、GRP 和 NMB,表现出广泛的药理/生物学反应。GRP 刺激平滑肌收缩和 GI 运动,释放大量 GI 激素/神经递质,以及胰腺、胃、结肠和许多内分泌器官的分泌和/或激素释放,并对免疫细胞具有有效作用,对正常组织和肿瘤的有效生长作用,有效的中枢神经系统作用,包括调节昼夜节律、体温调节;焦虑/恐惧反应、食物摄入和对胃肠道的众多中枢神经系统影响以及慢性瘙痒的脊髓传播。NMB引起平滑肌收缩,对各种组织有生长作用,具有中枢神经系统作用,包括摄食和体温调节作用,调节促甲状腺激素的释放,刺激各种中枢神经系统神经元,具有行为作用,对脊髓感觉传递有作用。GRP,在较小程度上影响 NMB,影响各种人类肿瘤的生长和/或分化,包括结肠癌、前列腺癌、肺癌和一些妇科癌症。敲除研究表明 BB(3) 在能量平衡、葡萄糖稳态、控制体重、肺发育和对损伤、肿瘤生长以及胃肠动力的反应。本综述总结了我们对这些受体的生物学/药理学理解的进展,包括它们的分类、结构、药理学、生理学和在病理生理条件下的作用。
更新日期:2019-11-01
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