Miyazaki Mitsunori, Takemasa Tohru
Department of Physical Therapy School of Rehabilitation Sciences Health Sciences University of Hokkaido Japan.
Graduate School of Comprehensive Human Sciences University of Tsukuba Ibaraki Japan.
FEBS Open Bio. 2017 Jan 30;7(3):424-433. doi: 10.1002/2211-5463.12195. eCollection 2017 Mar.
The enhanced rate of protein synthesis in skeletal muscle cells results in a net increase in total protein content that leads to skeletal muscle growth/hypertrophy. The mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK)-dependent regulation of the activity of mechanistic target of rapamycin (mTOR) and subsequent protein synthesis has been suggested as a regulatory mechanism; however, the exact molecular processes underlying such a regulation are poorly defined. The purpose of this study was to investigate regulatory mechanisms involved in the MEK/ERK-dependent pathway leading to mTORC1 activation in skeletal muscle cells. Treatment with phorbol-12-myristate-13-acetate (PMA), a potent agonist of protein kinase C (PKC) and its downstream effector in the MEK/ERK-dependent pathway, resulted in the activation of mTORC1 signaling and phosphorylation of the upstream regulator tuberous sclerosis 2 (TSC2) in C2C12 myoblasts. PMA-induced activation of mTORC1 signaling was partially prevented by treatment with U0126 (a selective inhibitor of MEK1/2) or BIX-02189 (a selective inhibitor of MEK5) and completely blocked with BIM-I (a selective inhibitor of upstream PKC). TSC2 phosphorylation at Ser664 (an ERK-dependent phosphorylation site) was prevented with U0126, and BIM-I treatment blocked PMA-induced phosphorylation of TSC2 at multiple residues (Ser664, Ser939, and Thr1462). Overexpression of Ras homolog enriched in brain (Rheb), a downstream target of TSC2, and an mTORC1 activator, was sufficient to activate mTORC1 signaling. We also identified that PMA-induced activation of mTORC1 signaling was significantly inhibited in the absence of Rheb with siRNA knockdown. These observations demonstrate that the PKC/MEK/ERK-dependent activation of mTORC1 is mediated through TSC2 phosphorylation and its downstream target Rheb in C2C12 myoblasts.
骨骼肌细胞中蛋白质合成速率的提高导致总蛋白质含量净增加,进而引起骨骼肌生长/肥大。有研究提出,丝裂原活化蛋白激酶激酶(MEK)/细胞外信号调节激酶(ERK)依赖性调节雷帕霉素作用机制靶点(mTOR)的活性及随后的蛋白质合成是一种调节机制;然而,这种调节背后的确切分子过程尚不清楚。本研究的目的是探讨参与MEK/ERK依赖性途径导致骨骼肌细胞中mTORC1激活的调节机制。用佛波醇-12-肉豆蔻酸酯-13-乙酸酯(PMA)处理,PMA是蛋白激酶C(PKC)及其在MEK/ERK依赖性途径中的下游效应物的强效激动剂,可导致C2C12成肌细胞中mTORC1信号激活和上游调节因子结节性硬化症2(TSC2)磷酸化。用U0126(MEK1/2的选择性抑制剂)或BIX-02189(MEK5的选择性抑制剂)处理可部分阻止PMA诱导的mTORC1信号激活,用BIM-I(上游PKC的选择性抑制剂)处理则可完全阻断。U0126可阻止Ser664(ERK依赖性磷酸化位点)处的TSC2磷酸化,BIM-I处理可阻断PMA诱导的TSC2在多个位点(Ser664、Ser939和Thr1462)的磷酸化。富含脑的Ras同源物(Rheb)是TSC2的下游靶点和mTORC1激活剂,其过表达足以激活mTORC1信号。我们还发现,通过小干扰RNA敲低使Rheb缺失时,PMA诱导的mTORC1信号激活受到显著抑制。这些观察结果表明,在C2C12成肌细胞中,PKC/MEK/ERK依赖性激活mTORC1是通过TSC2磷酸化及其下游靶点Rheb介导的。