Suppr超能文献

肾素原与(前体)肾素受体:来自啮齿动物体外研究和实验模型的现有数据综述

Prorenin and (pro)renin receptor: a review of available data from in vitro studies and experimental models in rodents.

作者信息

Nguyen Geneviève, Danser A H Jan

机构信息

Institut de la Santé et de la Recherche Médicale, (INSERM) Unit 833 and Collège de France, 11 place Marcelin Berthelot, 75005, Paris, France.

出版信息

Exp Physiol. 2008 May;93(5):557-63. doi: 10.1113/expphysiol.2007.040030. Epub 2008 Mar 30.

Abstract

The discovery of a (pro)renin receptor [(P)RR] and the introduction of renin inhibitors in the clinic have brought renin and prorenin back into the spotlight. The (P)RR binds both renin and its inactive precursor prorenin, and such binding triggers intracellular signalling that upregulates the expression of profibrotic genes, potentially leading to cardiac and renal fibrosis, growth and remodelling. Simultaneously, binding of renin to the (P)RR increases its angiotensin I-generating activity, whereas binding of prorenin allows the 'inactive' renin precursor to become fully enzymatically active. Therefore, the (pro)renin receptor system could be considered as having two functions, an angiotensin-independent function related to (P)RR-induced intracellular signalling and its downstream effects and an angiotensin-dependent function related to the increased catalytic activity of receptor-bound (pro)renin. A (P)RR blocker has already been described which blocks both functions, thus preventing diabetic nephropathy, cardiac fibrosis and ocular neovascularization. On-going experimental studies should now determine which of the two functions plays the more important role in pathological situations. The results of these studies are extremely important in view of the clinical use of renin inhibitors, since it is well known that their administration results in increased levels of both renin and prorenin. Although this rise can be interpreted as evidence of effective renin-angiotensin system blockade, it could also result in increased (P)RR activation.

摘要

(前)肾素受体[(P)RR]的发现以及肾素抑制剂在临床上的应用使肾素和肾素原再度成为焦点。(P)RR既能结合肾素,也能结合其无活性前体肾素原,这种结合会触发细胞内信号传导,从而上调促纤维化基因的表达,可能导致心脏和肾脏纤维化、生长及重塑。同时,肾素与(P)RR的结合会增加其生成血管紧张素I的活性,而肾素原的结合则使“无活性”的肾素前体完全具有酶活性。因此,(前)肾素受体系统可被视为具有两种功能,一种是与(P)RR诱导的细胞内信号传导及其下游效应相关的不依赖血管紧张素的功能,另一种是与受体结合的(前)肾素催化活性增加相关的依赖血管紧张素的功能。已经描述了一种(P)RR阻滞剂,它能阻断这两种功能,从而预防糖尿病肾病、心脏纤维化和眼部新生血管形成。目前正在进行的实验研究应确定这两种功能中的哪一种在病理情况下起更重要的作用。鉴于肾素抑制剂的临床应用,这些研究结果极其重要,因为众所周知,使用肾素抑制剂会导致肾素和肾素原水平升高。尽管这种升高可被解释为有效阻断肾素-血管紧张素系统的证据,但它也可能导致(P)RR激活增加。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验