Gromada J, Holst J J, Rorsman P
Department of Islet Cell Physiology, Novo Nordisk A/S, The Symbion Science Park, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
Pflugers Arch. 1998 Apr;435(5):583-94. doi: 10.1007/s004240050558.
Glucagon-like peptide 1 is a gastrointestinally derived hormone with profound effects on nutrient-induced pancreatic hormone release. GLP-1 modulates insulin, glucagon and somatostatin secretion by binding to guanine nucleotide binding protein-coupled receptors resulting in the activation of adenylate cyclase and generation of cyclic adenosine monophosphate (cAMP). In the B-cell, cAMP, via activation of protein kinase A, interacts with a plethora of signal transduction processes including ion channel activity, intracellular Ca2+ handling and exocytosis of the insulin-containing granules. The stimulatory action of GLP-1 on insulin secretion, contrary to that of the currently used hypoglycaemic sulphonylureas, is glucose dependent and requires the presence of normal or elevated concentrations of the sugar. For this reason, GLP-1 attracts much interest as a possible novel principle for the treatment of human type-2 diabetes. Here we review the actions of GLP-1 on islet cell function and attempt to integrate current knowledge into a working model for the control of pancreatic hormone secretion.
胰高血糖素样肽-1是一种源自胃肠道的激素,对营养物质诱导的胰腺激素释放具有深远影响。胰高血糖素样肽-1通过与鸟嘌呤核苷酸结合蛋白偶联受体结合,调节胰岛素、胰高血糖素和生长抑素的分泌,从而激活腺苷酸环化酶并生成环磷酸腺苷(cAMP)。在B细胞中,cAMP通过激活蛋白激酶A,与大量信号转导过程相互作用,包括离子通道活性、细胞内Ca2+处理以及含胰岛素颗粒的胞吐作用。与目前使用的降血糖磺酰脲类药物相反,胰高血糖素样肽-1对胰岛素分泌的刺激作用是葡萄糖依赖性的,并且需要存在正常或升高浓度的血糖。因此,胰高血糖素样肽-1作为治疗人类2型糖尿病的一种可能的新原理引起了广泛关注。在此,我们综述胰高血糖素样肽-1对胰岛细胞功能的作用,并尝试将当前知识整合到一个控制胰腺激素分泌的工作模型中。