Charité - Universitätsmedizin Berlin, Department of Internal Medicine and Cardiology, Berlin, Germany.
DZHK (German Centre for Cardiovascular Research), partner site Berlin, Berlin, Germany.
J Clin Invest. 2018 Jul 2;128(7):3024-3040. doi: 10.1172/JCI96477. Epub 2018 Jun 11.
Medial vascular calcification, associated with enhanced mortality in chronic kidney disease (CKD), is fostered by osteo-/chondrogenic transdifferentiation of vascular smooth muscle cells (VSMCs). Here, we describe that serum- and glucocorticoid-inducible kinase 1 (SGK1) was upregulated in VSMCs under calcifying conditions. In primary human aortic VSMCs, overexpression of constitutively active SGK1S422D, but not inactive SGK1K127N, upregulated osteo-/chondrogenic marker expression and activity, effects pointing to increased osteo-/chondrogenic transdifferentiation. SGK1S422D induced nuclear translocation and increased transcriptional activity of NF-κB. Silencing or pharmacological inhibition of IKK abrogated the osteoinductive effects of SGK1S422D. Genetic deficiency, silencing, and pharmacological inhibition of SGK1 dissipated phosphate-induced calcification and osteo-/chondrogenic transdifferentiation of VSMCs. Aortic calcification, stiffness, and osteo-/chondrogenic transdifferentiation in mice following cholecalciferol overload were strongly reduced by genetic knockout or pharmacological inhibition of Sgk1 by EMD638683. Similarly, Sgk1 deficiency blunted vascular calcification in apolipoprotein E-deficient mice after subtotal nephrectomy. Treatment of human aortic smooth muscle cells with serum from uremic patients induced osteo-/chondrogenic transdifferentiation, effects ameliorated by EMD638683. These observations identified SGK1 as a key regulator of vascular calcification. SGK1 promoted vascular calcification, at least partly, via NF-κB activation. Inhibition of SGK1 may, thus, reduce the burden of vascular calcification in CKD.
血管中层钙化与慢性肾脏病(CKD)患者死亡率增加相关,其发生是由血管平滑肌细胞(VSMCs)向成骨/软骨细胞的去分化所导致的。在这里,我们发现,在钙化条件下,VSMCs 中血清和糖皮质激素诱导的激酶 1(SGK1)表达上调。在原代人主动脉 VSMCs 中,组成型激活的 SGK1S422D 的过表达而非无活性的 SGK1K127N 的过表达,上调了成骨/软骨标志物的表达和活性,表明向成骨/软骨的去分化增加。SGK1S422D 诱导 NF-κB 的核易位和转录活性增加。IKK 的沉默或药理学抑制消除了 SGK1S422D 的成骨诱导作用。SGK1 的基因缺失、沉默和药理学抑制消除了磷酸盐诱导的 VSMCs 钙化和成骨/软骨的去分化。在维生素 D 过量负荷的小鼠中,敲除 Sgk1 或用 EMD638683 抑制 Sgk1 可强烈减少主动脉钙化、僵硬和向成骨/软骨的去分化。类似地,在接受部分肾切除的载脂蛋白 E 缺陷小鼠中,SGK1 缺乏也减弱了血管钙化。用尿毒症患者的血清处理人主动脉平滑肌细胞可诱导向成骨/软骨的去分化,这些作用可被 EMD638683 改善。这些观察结果确定了 SGK1 是血管钙化的关键调节因子。SGK1 通过 NF-κB 的激活促进血管钙化。因此,抑制 SGK1 可能会降低 CKD 患者的血管钙化负担。