Gekle M, Bretschneider M, Meinel S, Ruhs S, Grossmann C
Julius Bernstein Institute of Physiology, Martin Luther University Halle-Wittenberg, Germany.
Julius Bernstein Institute of Physiology, Martin Luther University Halle-Wittenberg, Germany.
Steroids. 2014 Mar;81:103-8. doi: 10.1016/j.steroids.2013.10.016. Epub 2013 Nov 16.
The mineralocorticoid receptor (MR) is a ligand-dependent transcription factor that physiologically regulates water-electrolyte homeostasis and controls blood pressure. The MR can also elicit inflammatory and remodeling processes in the cardiovascular system and the kidneys, which require the presence of additional pathological factors like for example nitrosative stress. However, the underlying molecular mechanism(s) for pathophysiological MR effects remain(s) elusive. The inactive MR is located in the cytosol associated with chaperone molecules including HSP90. After ligand binding, the MR monomer rapidly translocates into the nucleus while still being associated to HSP90 and after dissociation from HSP90 binds to hormone-response-elements called glucocorticoid response elements (GREs) as a dimer. There are indications that rapid MR trafficking is modulated in the presence of high salt, oxidative or nitrosative stress, hypothetically by induction or posttranslational modifications. Additionally, glucocorticoids and the enzyme 11beta hydroxysteroid dehydrogenase may also influence MR activation. Because MR trafficking and its modulation by micro-milieu factors influence MR cellular localization, it is not only relevant for genomic but also for nongenomic MR effects.
盐皮质激素受体(MR)是一种依赖配体的转录因子,在生理上调节水电解质平衡并控制血压。MR还可引发心血管系统和肾脏中的炎症和重塑过程,这需要存在额外的病理因素,例如亚硝化应激。然而,病理生理MR效应的潜在分子机制仍然难以捉摸。无活性的MR位于与包括HSP90在内的伴侣分子相关的细胞质中。配体结合后,MR单体迅速转运到细胞核中,同时仍与HSP90相关联,并在与HSP90解离后作为二聚体与称为糖皮质激素反应元件(GRE)的激素反应元件结合。有迹象表明,在高盐、氧化或亚硝化应激存在的情况下,快速的MR运输受到调节,推测是通过诱导或翻译后修饰。此外,糖皮质激素和11β羟类固醇脱氢酶也可能影响MR激活。由于MR运输及其受微环境因素的调节会影响MR的细胞定位,因此它不仅与基因组MR效应相关,也与非基因组MR效应相关。