Department of Medicine, University of Texas Health Science Center at San Antonio, San Antonio, Texas, United States of America.
PLoS One. 2012;7(8):e42316. doi: 10.1371/journal.pone.0042316. Epub 2012 Aug 3.
Transforming growth factor-β (TGFβ) promotes glomerular hypertrophy and matrix expansion, leading to glomerulosclerosis. MicroRNAs are well suited to promote fibrosis because they can repress gene expression, which negatively regulate the fibrotic process. Recent cellular and animal studies have revealed enhanced expression of microRNA, miR-21, in renal cells in response to TGFβ. Specific miR-21 targets downstream of TGFβ receptor activation that control cell hypertrophy and matrix protein expression have not been studied. Using 3'UTR-driven luciferase reporter, we identified the tumor suppressor protein PTEN as a target of TGFβ-stimulated miR-21 in glomerular mesangial cells. Expression of miR-21 Sponge, which quenches endogenous miR-21 levels, reversed TGFβ-induced suppression of PTEN. Additionally, miR-21 Sponge inhibited TGFβ-stimulated phosphorylation of Akt kinase, resulting in attenuation of phosphorylation of its substrate GSK3β. Tuberin and PRAS40, two other Akt substrates, and endogenous inhibitors of mTORC1, regulate mesangial cell hypertrophy. Neutralization of endogenous miR-21 abrogated TGFβ-stimulated phosphorylation of tuberin and PRAS40, leading to inhibition of phosphorylation of S6 kinase, mTOR and 4EBP-1. Moreover, downregulation of miR-21 significantly suppressed TGFβ-induced protein synthesis and hypertrophy, which were reversed by siRNA-targeted inhibition of PTEN expression. Similarly, expression of constitutively active Akt kinase reversed the miR-21 Sponge-mediated inhibition of TGFβ-induced protein synthesis and hypertrophy. Furthermore, expression of constitutively active mTORC1 prevented the miR-21 Sponge-induced suppression of mesangial cell protein synthesis and hypertrophy by TGFβ. Finally, we show that miR-21 Sponge inhibited TGFβ-stimulated fibronectin and collagen expression. Suppression of PTEN expression and expression of both constitutively active Akt kinase and mTORC1 independently reversed this miR-21-mediated inhibition of TGFβ-induced fibronectin and collagen expression. Our results uncover an essential role of TGFβ-induced expression of miR-21, which targets PTEN to initiate a non-canonical signaling circuit involving Akt/mTORC1 axis for mesangial cell hypertrophy and matrix protein synthesis.
转化生长因子-β(TGFβ)可促进肾小球肥大和基质扩张,导致肾小球硬化。 microRNA 非常适合促进纤维化,因为它们可以抑制基因表达,从而负调控纤维化过程。最近的细胞和动物研究表明,TGFβ 可增强肾脏细胞中 microRNA,miR-21 的表达。尚未研究控制细胞肥大和基质蛋白表达的 TGFβ 受体激活下游特定的 miR-21 靶标。使用 3'UTR 驱动的荧光素酶报告基因,我们鉴定出肿瘤抑制蛋白 PTEN 是肾小球系膜细胞中 TGFβ 刺激的 miR-21 的靶标。miR-21 Sponge 的表达可抑制内源性 miR-21 水平,逆转 TGFβ 诱导的 PTEN 抑制。此外,miR-21 Sponge 抑制 TGFβ 刺激的 Akt 激酶磷酸化,导致其底物 GSK3β 磷酸化的衰减。Akt 的另外两个底物 tuberin 和 PRAS40 以及 mTORC1 的内源性抑制剂,调节系膜细胞肥大。内源性 miR-21 的中和消除了 TGFβ 刺激的 tuberin 和 PRAS40 的磷酸化,导致 S6 激酶、mTOR 和 4EBP-1 的磷酸化抑制。此外,下调 miR-21 显著抑制 TGFβ 诱导的蛋白合成和肥大,这可通过针对 PTEN 表达的 siRNA 靶向抑制来逆转。同样,组成型激活 Akt 激酶的表达逆转了 miR-21 Sponge 介导的 TGFβ 诱导的蛋白合成和肥大抑制。此外,组成型激活 mTORC1 可防止 miR-21 Sponge 抑制 TGFβ 诱导的系膜细胞蛋白合成和肥大。最后,我们表明 miR-21 Sponge 抑制 TGFβ 刺激的纤连蛋白和胶原蛋白表达。PTEN 表达的抑制以及组成型激活的 Akt 激酶和 mTORC1 的表达均可独立逆转这种 miR-21 介导的 TGFβ 诱导的纤连蛋白和胶原蛋白表达抑制。我们的结果揭示了 TGFβ 诱导的 miR-21 表达的重要作用,该表达靶向 PTEN 以启动涉及 Akt/mTORC1 轴的非典型信号通路,用于系膜细胞肥大和基质蛋白合成。