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肿瘤中的生长抑素、促皮质素释放因子及其受体。

Somatostatin, cortistatin and their receptors in tumours.

作者信息

Volante M, Rosas R, Allìa E, Granata R, Baragli A, Muccioli G, Papotti M

机构信息

Department of Clinical & Biological Sciences, University of Turin at San Luigi Hospital, Orbassano, University of Turin, Torino, Italy.

出版信息

Mol Cell Endocrinol. 2008 May 14;286(1-2):219-29. doi: 10.1016/j.mce.2007.12.002. Epub 2007 Dec 8.

Abstract

Somatostatin (SS) and its synthetic analogs have a role in the treatment of neuroendocrine tumours both in terms of symptoms control and antiproliferative activities. These effects are mediated by five SS receptors, widely expressed in both human neuroendocrine and non-neuroendocrine tumours, which were demonstrated to be diagnostically and therapeutically valuable targets. Cortistatin (CST), a brain cortex peptide, partially homologous to SS and having similar functions is also expressed in peripheral tissues and tumours. CST binds all SS receptors, and, differently from SS, also the ghrelin receptor GHSR1a and the CST specific receptor MrgX2. The expression profile of CST is mostly restricted to neuroendocrine tumours (gastrointestinal, pancreas, lung, parathyroid, thyroid, adrenal). In these tumours, CST probably acts via the SS or ghrelin receptor, the MrgX2 receptor being absent. Thus, in comparison to SS analogs, CST synthetic analogs may represent additional diagnostic/therapeutic tools in those tumours expressing the receptors for SS, for ghrelin or for both peptides.

摘要

生长抑素(SS)及其合成类似物在神经内分泌肿瘤的治疗中,在症状控制和抗增殖活性方面均发挥作用。这些作用是由五种SS受体介导的,它们在人类神经内分泌肿瘤和非神经内分泌肿瘤中广泛表达,已被证明是具有诊断和治疗价值的靶点。可体抑素(CST)是一种大脑皮质肽,与SS部分同源且功能相似,也在外周组织和肿瘤中表达。CST可结合所有SS受体,与SS不同的是,它还可结合胃饥饿素受体GHSR1a和CST特异性受体MrgX2。CST的表达谱大多局限于神经内分泌肿瘤(胃肠道、胰腺、肺、甲状旁腺、甲状腺、肾上腺)。在这些肿瘤中,CST可能通过SS或胃饥饿素受体发挥作用,因为不存在MrgX2受体。因此,与SS类似物相比,CST合成类似物可能是那些表达SS受体、胃饥饿素受体或两种肽类受体的肿瘤中额外的诊断/治疗工具。

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