Division of Endocrinology and Metabolism, Dept. of Medicine III, Medical University of Vienna, Waehringer Guertel 18-20, Vienna, Austria.
Am J Physiol Endocrinol Metab. 2011 Aug;301(2):E336-41. doi: 10.1152/ajpendo.00155.2011. Epub 2011 May 17.
Serum- and glucocorticoid-regulated kinase-1 (SGK1) is a glucocorticoid early-response gene; its function, however, has been elucidated mainly in the context of mineralocorticoid signaling. Here, we investigate the expression and function of SGK1 in the pituitary gland, one of the primary glucocorticoid targets. SGK1 is expressed in the human pituitary gland and colocalizes to ACTH. The AtT-20 murine corticotroph cell line was used for functional experiments. Glucocorticoids upregulated SGK1 mRNA and protein levels, parallel to decreasing proopiomelanocortin (POMC) transcription and ACTH release. Dexamethasone-induced changes in SGK1 protein were abolished by the steroid receptor antagonist RU-486 and reduced by the inhibition of PI 3-kinase with LY-294002. SGK1 overexpression increased CREB- and activator protein-1-dependent transcription, POMC transcription, and ACTH secretion but did not influence intracellular cAMP levels. SGK1 overexpression and corticotropin-releasing hormone had additive effects on POMC promoter activity but not on ACTH secretion. SGK1 knockdown by RNA interference decreased POMC promoter activity, demonstrating the importance of SGK1 for basal POMC signaling. In summary, SGK1 is strongly stimulated by glucocorticoids in pituitary corticotrophs; however, its effects on POMC transcription are antagonistic to the classical inhibitory glucocorticoid action, suggesting a cell-regulated counterregulatory mechanism to potentially detrimental glucocorticoid effects.
血清和糖皮质激素调节激酶 1(SGK1)是一种糖皮质激素早期反应基因;然而,其功能主要在醛固酮信号转导的背景下得到阐明。在这里,我们研究了 SGK1 在垂体中的表达和功能,垂体是糖皮质激素的主要靶器官之一。SGK1 在人垂体中表达,并与 ACTH 共定位。使用 AtT-20 鼠 corticotroph 细胞系进行功能实验。糖皮质激素上调 SGK1 mRNA 和蛋白水平,与促肾上腺皮质激素释放激素(POMC)转录和 ACTH 释放减少平行。类固醇受体拮抗剂 RU-486 可消除地塞米松诱导的 SGK1 蛋白变化,并通过 PI 3-激酶抑制剂 LY-294002 减少其变化。SGK1 的过表达增加了 CREB 和激活蛋白-1 依赖性转录、POMC 转录和 ACTH 分泌,但不影响细胞内 cAMP 水平。SGK1 的过表达和促肾上腺皮质激素释放激素对 POMC 启动子活性具有相加作用,但对 ACTH 分泌没有影响。通过 RNA 干扰的 SGK1 敲低降低了 POMC 启动子活性,表明 SGK1 对基础 POMC 信号传导很重要。总之,SGK1 在垂体 corticotrophs 中受到糖皮质激素的强烈刺激;然而,其对 POMC 转录的影响与经典的抑制性糖皮质激素作用相反,表明存在一种细胞调节的代偿性机制,以潜在地对抗糖皮质激素的有害作用。