Division of Brain Disease, Center for Biomedical Science, National Institutes of Health, Korea Center for Disease Control and Prevention, 187 Osongsaengmyeong2-ro, Gangoe-myeon, Cheongwon-gun, Chungcheongbuk-do 363-951, South Korea.
J Biol Chem. 2011 May 27;286(21):18903-13. doi: 10.1074/jbc.M111.225128. Epub 2011 Mar 30.
Previously, we reported that mitogen-activated protein kinase kinase 1 (MEK1) activated in the mid-stage of skeletal muscle differentiation promotes myogenic differentiation. To elucidate the molecular mechanism, we investigated an activity of MEK1 for MyoD. Activated MEK1 associates with MyoD in the nucleus of differentiating myoblasts. In vitro kinase assay using active MEK1, a (32)P-labeled protein band corresponding to GST-MyoD was observed but not to mutant GST-MyoD-Y156F. Tyrosine phosphorylation of endogenous MyoD was detected with a specific anti-pMyoD-Y156 antibody; however, this response was blocked by PD184352, a MEK-specific inhibitor. These results indicate that activated MEK1 phosphorylates the MyoD-Y156 residue directly. Interestingly, the protein level of mutant MyoD-Y156F decreased compared with that of wild type but was recovered in the presence of lactacystin, a proteasome inhibitor. The protein level of MyoD-Y156E, which mimics phosphorylation at Tyr-156, was above that of wild type, indicating that the phosphorylation protects MyoD from the ubiquitin proteasome-mediated degradation. In addition, the low protein level of MyoD-Y156F was recovered over that of wild type by an additional mutation at Leu-164, a critical binding residue of MAFbx/AT-1, a Skp, Cullin, F-box (SCF) E3-ubiquitin ligase. The amount of MyoD co-precipitated with MAFbx/AT-1 also was reduced in the presence of active MEK1. Thus, these results suggested that the phosphorylation probably interrupts the binding of MAFbx/AT-1 to MyoD and thereby increases its stability. Collectively, our results suggest that MEK1 activated in differentiating myoblasts stimulates muscle differentiation by phosphorylating MyoD-Y156, which results in MyoD stabilization.
先前,我们报道过在骨骼肌分化的中期被激活的丝裂原活化蛋白激酶激酶 1(MEK1)可促进成肌分化。为了阐明其分子机制,我们研究了 MEK1 对 MyoD 的活性。在分化的肌母细胞的核中,激活的 MEK1 与 MyoD 结合。使用活性 MEK1 进行的体外激酶测定中,观察到与 GST-MyoD 相对应的(32)P 标记蛋白带,但与突变 GST-MyoD-Y156F 不对应。用特异性抗 pMyoD-Y156 抗体检测到内源性 MyoD 的酪氨酸磷酸化;然而,该反应被 MEK 特异性抑制剂 PD184352 阻断。这些结果表明激活的 MEK1 直接磷酸化 MyoD-Y156 残基。有趣的是,与野生型相比,突变型 MyoD-Y156F 的蛋白水平降低,但在蛋白酶体抑制剂乳香酰环丙氨酸存在的情况下恢复。模拟 Tyr-156 磷酸化的 MyoD-Y156E 的蛋白水平高于野生型,表明磷酸化使 MyoD 免受泛素蛋白酶体介导的降解。此外,通过在 Leu-164 上的另一个突变(MAFbx/AT-1 的关键结合残基,Skp、Cullin、F-box(SCF)E3-泛素连接酶),MyoD-Y156F 的低蛋白水平也恢复到高于野生型的水平。与 MAFbx/AT-1 共沉淀的 MyoD 量也在活性 MEK1 的存在下减少。因此,这些结果表明,磷酸化可能中断 MAFbx/AT-1 与 MyoD 的结合,从而增加其稳定性。总的来说,我们的结果表明,在分化的肌母细胞中被激活的 MEK1 通过磷酸化 MyoD-Y156 来刺激肌肉分化,从而导致 MyoD 稳定。