Bandyopadhyay G, Standaert M L, Galloway L, Moscat J, Farese R V
J. A. Haley Veterans Hospital and the Department of Internal Medicine, University of South Florida College of Medicine, Tampa 33612, USA.
Endocrinology. 1997 Nov;138(11):4721-31. doi: 10.1210/endo.138.11.5473.
We examined the question of whether insulin activates protein kinase C (PKC)-zeta in L6 myotubes, and the dependence of this activation on phosphatidylinositol (PI) 3-kinase. We also evaluated a number of issues that are relevant to the question of whether diacylglycerol (DAG)-dependent PKCs or DAG-insensitive PKCs, such as PKC-zeta, are more likely to play a role in insulin-stimulated glucose transport in L6 myotubes and other insulin-sensitive cell types. We found that insulin increased the enzyme activity of immunoprecipitable PKC-zeta in L6 myotubes, and this effect was blocked by PI 3-kinase inhibitors, wortmannin and LY294002; this suggested that PKC-zeta operates downstream of PI 3-kinase during insulin action. We also found that treatment of L6 myotubes with 5 microM tetradecanoyl phorbol-13-acetate (TPA) for 24 h led to 80-100% losses of all DAG-dependent PKCs (alpha, beta1, beta2, delta, epsilon) and TPA-stimulated glucose transport (2-deoxyglucose uptake); in contrast, there was full retention of PKC-zeta, as well as insulin-stimulated glucose transport and translocation of GLUT4 and GLUT1 to the plasma membrane. Unlike what has been reported in BC3H-1 myocytes, TPA treatment did not elicit increases in PKCbeta2 messenger RNA or protein in L6 myotubes, and selective retention of this PKC isoform could not explain the retention of insulin effects on glucose transport after prolonged TPA treatment. Of further interest, TPA acutely activated membrane-associated PI 3-kinase in L6 myotubes, and acute effects of TPA on glucose transport were inhibited, not only by the PKC inhibitor, LY379196, but also by both wortmannin and LY294002; this suggested that DAG-sensitive PKCs activate glucose transport through cross-talk with phosphatidylinositol (PI) 3-kinase, rather than directly through PKC. Also, the cell-permeable, myristoylated PKC-zeta pseudosubstrate inhibited insulin-stimulated glucose transport both in non-down-regulated and PKC-depleted (TPA-treated) L6 myotubes; thus, the PKC-zeta pseudosubstrate appeared to inhibit a protein kinase that is required for insulin-stimulated glucose transport but is distinct from DAG-sensitive PKCs. In keeping with the latter dissociation of DAG-sensitive PKCs and insulin-stimulated glucose transport, LY379196, which inhibits PKC-beta (preferentially) and other DAG-sensitive PKCs at relatively low concentrations, inhibited insulin-stimulated glucose transport only at much higher concentrations, not only in L6 myotubes, but also in rat adipocytes, BC3H-1 myocytes, 3T3/L1 adipocytes and rat soleus muscles. Finally, stable and transient expression of a kinase-inactive PKC-zeta inhibited basal and insulin-stimulated glucose transport in L6 myotubes. Collectively, our findings suggest that, whereas PKC-zeta is a reasonable candidate to participate in insulin stimulation of glucose transport, DAG-sensitive PKCs are unlikely participants.
我们研究了胰岛素是否能激活L6肌管中的蛋白激酶C(PKC)-ζ,以及这种激活对磷脂酰肌醇(PI)3激酶的依赖性。我们还评估了一些与以下问题相关的问题:二酰基甘油(DAG)依赖性PKC或DAG不敏感的PKC(如PKC-ζ)是否更有可能在L6肌管和其他胰岛素敏感细胞类型的胰岛素刺激的葡萄糖转运中发挥作用。我们发现胰岛素增加了L6肌管中可免疫沉淀的PKC-ζ的酶活性,并且这种作用被PI 3激酶抑制剂渥曼青霉素和LY294002阻断;这表明在胰岛素作用过程中PKC-ζ在PI 3激酶的下游发挥作用。我们还发现,用5微摩尔十四酰佛波醇-13-乙酸酯(TPA)处理L6肌管24小时导致所有DAG依赖性PKC(α、β1、β2、δ、ε)损失80 - 100%,以及TPA刺激的葡萄糖转运(2-脱氧葡萄糖摄取);相反,PKC-ζ完全保留,以及胰岛素刺激的葡萄糖转运和GLUT4及GLUT1向质膜的转位。与在BC3H-1肌细胞中报道的情况不同,TPA处理未引起L6肌管中PKCβ2信使RNA或蛋白质增加,并且这种PKC同工型的选择性保留不能解释长时间TPA处理后胰岛素对葡萄糖转运的作用的保留。更有趣的是,TPA在L6肌管中急性激活膜相关的PI 3激酶,并且TPA对葡萄糖转运的急性作用不仅被PKC抑制剂LY379196抑制,而且被渥曼青霉素和LY294002抑制;这表明DAG敏感的PKC通过与磷脂酰肌醇(PI)3激酶的相互作用激活葡萄糖转运,而不是直接通过PKC。此外,细胞可渗透的、肉豆蔻酰化的PKC-ζ假底物在未下调和PKC缺失(TPA处理)的L6肌管中均抑制胰岛素刺激的葡萄糖转运;因此,PKC-ζ假底物似乎抑制了胰岛素刺激的葡萄糖转运所需的一种蛋白激酶,但不同于DAG敏感的PKC。与DAG敏感的PKC和胰岛素刺激的葡萄糖转运的后者分离一致,LY379196在相对低浓度下优先抑制PKC-β和其他DAG敏感的PKC,仅在高得多的浓度下抑制胰岛素刺激的葡萄糖转运,不仅在L6肌管中,而且在大鼠脂肪细胞、BC3H-1肌细胞、3T3/L1脂肪细胞和大鼠比目鱼肌中。最后,激酶失活的PKC-ζ的稳定和瞬时表达抑制了L6肌管中的基础和胰岛素刺激的葡萄糖转运。总体而言,我们的发现表明,虽然PKC-ζ是参与胰岛素刺激葡萄糖转运的合理候选者,但DAG敏感型PKC不太可能参与其中。