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黏附 G 蛋白偶联受体广泛表达于胃肠道各节段。

Adhesion GPCRs are widely expressed throughout the subsections of the gastrointestinal tract.

机构信息

Department of Neuroscience, Uppsala University, BMC, Uppsala, SE 75124, Sweden.

出版信息

BMC Gastroenterol. 2012 Sep 25;12:134. doi: 10.1186/1471-230X-12-134.

Abstract

BACKGROUND

G protein-coupled receptors (GPCRs) represent one of the largest families of transmembrane receptors and the most common drug target. The Adhesion subfamily is the second largest one of GPCRs and its several members are known to mediate neural development and immune system functioning through cell-cell and cell-matrix interactions. The distribution of these receptors has not been characterized in detail in the gastrointestinal (GI) tract. Here we present the first comprehensive anatomical profiling of mRNA expression of all 30 Adhesion GPCRs in the rat GI tract divided into twelve subsegments.

METHODS

Using RT-qPCR, we studied the expression of Adhesion GPCRs in the esophagus, the corpus and antrum of the stomach, the proximal and distal parts of the duodenum, ileum, jejunum and colon, and the cecum.

RESULTS

We found that twenty-one Adhesion GPCRs (70%) had a widespread (expressed in five or more segments) or ubiquitous (expressed in eleven or more segments) distribution, seven (23%) were restricted to a few segments of the GI tract and two were not expressed in any segment. Most notably, almost all Group III members were ubiquitously expressed, while the restricted expression was characteristic for the majority of group VII members, hinting at more specific/localized roles for some of these receptors.

CONCLUSIONS

Overall, the distribution of Adhesion GPCRs points to their important role in GI tract functioning and defines them as a potentially crucial target for pharmacological interventions.

摘要

背景

G 蛋白偶联受体(GPCRs)是最大的跨膜受体家族之一,也是最常见的药物靶点。黏附亚家族是 GPCRs 中第二大亚家族,其几个成员已知通过细胞-细胞和细胞-基质相互作用来介导神经发育和免疫系统功能。这些受体在胃肠道(GI)中的分布尚未详细描述。在这里,我们首次全面分析了大鼠 GI 道中 30 种黏附 GPCR 的 mRNA 表达谱,将其分为 12 个亚段。

方法

使用 RT-qPCR,我们研究了食道、胃体和胃窦、十二指肠近端和远端、回肠、空肠和结肠以及盲肠中黏附 GPCR 的表达。

结果

我们发现 21 种黏附 GPCR(70%)具有广泛(在 5 个或更多段中表达)或普遍(在 11 个或更多段中表达)的分布,7 种(23%)局限于 GI 道的少数段,2 种在任何段都不表达。值得注意的是,几乎所有的第三组成员都普遍表达,而大多数第七组成员的表达受到限制,这暗示了这些受体中的一些具有更特定/局部的作用。

结论

总体而言,黏附 GPCR 的分布表明它们在 GI 道功能中的重要作用,并将其定义为潜在的药物干预的关键靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94e3/3526421/05a9c89d8a6c/1471-230X-12-134-1.jpg

相似文献

9
Adhesion-GPCRs: emerging roles for novel receptors.黏附G蛋白偶联受体:新型受体的新作用
Trends Biochem Sci. 2008 Oct;33(10):491-500. doi: 10.1016/j.tibs.2008.07.005. Epub 2008 Sep 11.

本文引用的文献

1
Trends in the exploitation of novel drug targets.新型药物靶点的开发趋势。
Nat Rev Drug Discov. 2011 Aug 1;10(8):579-90. doi: 10.1038/nrd3478.

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