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[5种克隆的人类生长抑素受体的分子生物学、药理学及信号转导]

[Molecular biology, pharmacology and signal transduction of 5 cloned human somatostatin receptors].

作者信息

Fehmann H C, Arnold R

机构信息

Abteilung für Gastroenterologie und Endokrinologie, Philipps-Universität Marburg.

出版信息

Z Gastroenterol. 1996 Nov;34(11):767-74.

PMID:9045539
Abstract

Somatostatin is a hormone with inhibitory properties, which is expressed in several tissues including the gastrointestinal tract. Actually, somatostatin and somatostatin-analogues are used for the treatment of neuroendocrine tumors and esophageal varices. Somatostatin acts via specific receptors. So far, five somatostatin receptor subtypes have been isolated and cloned. They are characterized by a high degree of sequence homology. The different receptor subtypes recognize the naturally occurring and the pharmaceutically developed ligands with different affinities. The receptor subtypes are expressed in a tissue-specific manner and in different tissues they couple to different signal-transduction pathways. The somatostatin receptors are also expressed in several malignant tissues. But the expression pattern varies from tumor to tumor. The availability of the receptors and their cDNAs allows the characterization of somatostatin's molecular action in greater detail. The design of even more potent somatostatin anlogues seems possible as well as the development of new therapeutical strategies.

摘要

生长抑素是一种具有抑制特性的激素,它在包括胃肠道在内的多种组织中表达。实际上,生长抑素及其类似物被用于治疗神经内分泌肿瘤和食管静脉曲张。生长抑素通过特定受体发挥作用。到目前为止,已分离并克隆出五种生长抑素受体亚型。它们的特点是具有高度的序列同源性。不同的受体亚型以不同的亲和力识别天然存在的和药物研发的配体。受体亚型以组织特异性方式表达,并且在不同组织中它们与不同的信号转导途径偶联。生长抑素受体也在多种恶性组织中表达。但表达模式因肿瘤而异。受体及其cDNA的可得性使得能够更详细地描述生长抑素的分子作用。设计更有效的生长抑素类似物以及开发新的治疗策略似乎也是可能的。

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