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Amylin: Pharmacology, Physiology, and Clinical Potential

机译:Amylin:药理学,生理学和临床潜力

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摘要

Amylin is a pancreatic β-cell hormone that produces effects in several different organ systems. Here, we review the literature in rodents and in humans on amylin research since its discovery as a hormone about 25 years ago. Amylin is a 37-amino-acid peptide that activates its specific receptors, which are multisubunit G protein-coupled receptors resulting from the coexpression of a core receptor protein with receptor activity-modifying proteins, resulting in multiple receptor subtypes. Amylin's major role is as a glucoregulatory hormone, and it is an important regulator of energy metabolism in health and disease. Other amylin actions have also been reported, such as on the cardiovascular system or on bone. Amylin acts principally in the circumventricular organs of the central nervous system and functionally interacts with other metabolically active hormones such as cholecystokinin, leptin, and estradiol. The amylin-based peptide, pramlintide, is used clinically to treat type 1 and type 2 diabetes. Clinical studies in obesity have shown that amylin agonists could also be useful for weight loss, especially in combination with other agents.
机译:胰岛淀粉样多肽是一种胰腺β细胞激素,可在几种不同的器官系统中产生作用。在这里,我们回顾了淀粉糊精研究以来关于啮齿动物和人类的文献,因为淀粉糊精是大约25年前被发现的一种激素。胰岛淀粉样多肽是激活其特异性受体的37个氨基酸的肽,特异性受体是多亚基G蛋白偶联的受体,是核心受体蛋白与受体活性修饰蛋白的共表达导致的多种受体亚型。胰岛淀粉样多肽的主要作用是作为糖调节激素,它是健康和疾病中能量代谢的重要调节剂。还报道了其他胰岛淀粉样多肽作用,例如在心血管系统或骨骼上。胰岛淀粉样多肽主要作用于中枢神经系统的脑室,并与其他代谢活性激素(如胆囊收缩素,瘦素和雌二醇)发生功能性相互作用。基于胰岛淀粉样多肽的普兰林肽在临床上用于治疗1型和2型糖尿病。肥胖症的临床研究表明,胰岛淀粉样多肽激动剂也可用于减肥,特别是与其他药物联用时。

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