Department of Pharmacology, Metabolic Diseases and Cell Signaling Laboratory, Research Institute for Medical Sciences, Chungnam National University School of Medicine, Daejeon, 301-747, South Korea.
Brain Res. 2013 Oct 2;1533:37-43. doi: 10.1016/j.brainres.2013.08.028. Epub 2013 Aug 22.
3-phosphoinositide-dependent kinase-1 (PDK1) is suggested to play important roles in the regulation of synaptic plasticity and neuronal cell survival in the mature CNS. Although few studies have investigated the roles of PDK1, little is known about PDK1 changes in glial cells under neuropathological conditions. In current report, phosphorylation of PDK1 was monitored specially on tyrosine residues, following the induction of an excitotoxic lesion in rat brain by using kainic acid administration. In injured hippocampal CA3 region, Tyr9 phosphorylation of PDK1 was increased from 4h until 3 day post-injection. Double immunohistochemistry further evaluated that these phosphorylated forms of PDK1 were localized in astrocytes not other cells. Overexpression of unphosphorylatable mutant, PDK1-Y9F leads to inhibit Protein kinase B (PKB/Akt) activation and cAMP responsive element binding protein (CREB) phosphorylation. In conclusion, our results suggested for the first time that tyrosine phosphorylation of PDK1 is required for PKB and CREB activation in KA-mediated excitotoxic lesion in mouse brain.
3-磷酸肌醇依赖的激酶-1(PDK1)被认为在成熟中枢神经系统中调节突触可塑性和神经元细胞存活方面发挥重要作用。尽管很少有研究探讨 PDK1 的作用,但在神经病理条件下,关于神经胶质细胞中 PDK1 的变化知之甚少。在本报告中,使用海人酸(kainic acid)处理诱导大鼠大脑兴奋性损伤,专门监测 PDK1 在酪氨酸残基上的磷酸化。在损伤的海马 CA3 区,PDK1 的 Tyr9 磷酸化从注射后 4 小时增加到 3 天。双重免疫组织化学进一步评估表明,这些磷酸化形式的 PDK1 定位于星形胶质细胞而不是其他细胞。过表达非磷酸化突变体 PDK1-Y9F 会抑制蛋白激酶 B(PKB/Akt)和 cAMP 反应元件结合蛋白(CREB)的磷酸化。总之,我们的结果首次表明,在 KA 介导的小鼠大脑兴奋性损伤中,PDK1 的酪氨酸磷酸化是 PKB 和 CREB 激活所必需的。