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胃肠道生理学中的G蛋白偶联受体。I. 胆囊收缩素受体:一个典型的家族。

G protein-coupled receptors in gastrointestinal physiology. I. CCK receptors: an exemplary family.

作者信息

Wank S A

机构信息

Digestive Diseases Branch, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-1804, USA.

出版信息

Am J Physiol. 1998 Apr;274(4 Pt 1):G607-13. doi: 10.1152/ajpgi.1998.274.4.g607.

DOI:10.1152/ajpgi.1998.274.4.g607
PMID:9575840
Abstract

The CCK and gastrin families of peptides act as hormones and neuropeptides on central and peripheral receptors to mediate secretion and motility in the gastrointestinal tract in the physiological response to a normal meal. Thus far, two CCK receptors have been molecularly identified to mediate the actions of CCK and gastrin, CCK-A and CCK-B receptors (CCK-AR and CCK-BR, respectively). The regulation of CCK-AR and CCK-BR affinity by guanine nucleotides and the receptor activation of G protein-dependent stimulation of phospholipase C and adenylyl cyclase suggested that they were guanine nucleotide-binding protein-coupled receptors [G protein-coupled receptors (GPCRs)]; however, the eventual cloning of their cDNAs revealed their heptahelical structure and confirmed their membership in the GPCR superfamily. The gastrointestinal system is a rich source of neuroendocrine hormones that interact with a large number of GPCRs to regulate the complex tasks of digestion, absorption, and excretion of a meal. This article focuses on the CCK family of GPCRs, and its activities in the gastrointestinal system.

摘要

缩胆囊素(CCK)和胃泌素肽家族作为激素和神经肽作用于中枢和外周受体,在对正常餐食的生理反应中调节胃肠道的分泌和运动。到目前为止,已从分子水平鉴定出两种介导CCK和胃泌素作用的CCK受体,即CCK-A和CCK-B受体(分别为CCK-AR和CCK-BR)。鸟嘌呤核苷酸对CCK-AR和CCK-BR亲和力的调节以及G蛋白依赖性刺激磷脂酶C和腺苷酸环化酶的受体激活表明它们是鸟嘌呤核苷酸结合蛋白偶联受体[G蛋白偶联受体(GPCRs)];然而,它们cDNA的最终克隆揭示了它们的七螺旋结构,并证实它们属于GPCR超家族。胃肠系统是神经内分泌激素的丰富来源,这些激素与大量GPCR相互作用,以调节餐食消化、吸收和排泄的复杂任务。本文重点关注GPCR的CCK家族及其在胃肠系统中的活性。

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