Simoncini Tommaso, Mannella Paolo, Fornari Letizia, Caruso Antonella, Varone Gaetano, Genazzani Andrea Riccardo
Molecular and Cellular Gynecological Endocrinology Laboratory (MCGEL), Department of Reproductive Medicine and Child Development, Division of Obstetrics and Gynecology, University of Pisa, Via Roma 67, 56100 Pisa, Italy.
Steroids. 2004 Aug;69(8-9):537-42. doi: 10.1016/j.steroids.2004.05.009.
Estrogen receptors act via the regulation of transcriptional processes, involving nuclear translocation and binding on specific response elements, thus leading to regulation of target gene expression. However, novel non-transcriptional mechanisms of signal transduction through steroid hormone receptors have been identified. These so-called "non-genomic" effects are independent by gene transcription or protein synthesis and involve steroid-induced modulation of cytoplasmic or of cell membrane-bound regulatory proteins. Relevant biological actions of steroids have been associated with this signaling in different tissues. Ubiquitary regulatory cascades such as mitogen-activated protein kinases (MAPK), the phosphatidylinositol 3-OH kinase (PI3K) and tyrosine kinases are modulated through non-transcriptional mechanisms by steroid hormones. Furthermore, steroid hormone receptors modulation of cell membrane-associated molecules such as ion channels and G-protein-coupled receptors has been shown in diverse tissues. The vascular wall is a site where non-genomic steroid hormones actions are particularly prominent. For instance, estrogens and glucocorticoids trigger rapid vasodilatation due to rapid induction of nitric oxide synthesis in endothelial cells via the estrogen receptor-dependent activation of MAPK and PI3K, leading to relevant pathophysiological consequences, in vitro and in vivo. The growing amount of evidence collected in the last years claims that non-transcriptional signaling mechanisms play a primary role in the generation of the effects of steroids on endothelial cells, which may turn out to be of relevance for clinical purposes.
雌激素受体通过调节转录过程发挥作用,包括核转位以及与特定反应元件结合,从而调控靶基因的表达。然而,现已发现类固醇激素受体信号转导的新型非转录机制。这些所谓的“非基因组”效应独立于基因转录或蛋白质合成,涉及类固醇诱导的细胞质或细胞膜结合调节蛋白的调控。类固醇的相关生物学作用已与不同组织中的这种信号传导相关联。诸如丝裂原活化蛋白激酶(MAPK)、磷脂酰肌醇3 - 羟基激酶(PI3K)和酪氨酸激酶等普遍存在的调节级联反应可通过类固醇激素的非转录机制进行调节。此外,在多种组织中已显示类固醇激素受体对细胞膜相关分子如离子通道和G蛋白偶联受体具有调节作用。血管壁是类固醇激素非基因组作用特别突出的部位。例如,雌激素和糖皮质激素可通过雌激素受体依赖性激活MAPK和PI3K,在内皮细胞中快速诱导一氧化氮合成,从而引发快速血管舒张,在体外和体内均会导致相关的病理生理后果。近年来收集的越来越多的证据表明,非转录信号传导机制在类固醇对内皮细胞作用的产生中起主要作用,这可能对临床应用具有重要意义。