Hoeflich K P, Luo J, Rubie E A, Tsao M S, Jin O, Woodgett J R
Ontario Cancer Institute/Princess Margaret Hospital, Toronto, Canada.
Nature. 2000 Jul 6;406(6791):86-90. doi: 10.1038/35017574.
Glycogen synthase kinase-3 (GSK-3)-alpha and -beta are closely related protein-serine kinases, which act as inhibitory components of Wnt signalling during embryonic development and cell proliferation in adult tissues. Insight into the physiological function of GSK-3 has emerged from genetic analysis in Drosophila, Dictyostelium and yeast. Here we show that disruption of the murine GSK-3beta gene results in embryonic lethality caused by severe liver degeneration during mid-gestation, a phenotype consistent with excessive tumour necrosis factor (TNF) toxicity, as observed in mice lacking genes involved in the activation of the transcription factor activation NF-kappaB. GSK-3beta-deficient embryos were rescued by inhibition of TNF using an anti-TNF-alpha antibody. Fibroblasts from GSK-3beta-deficient embryos were hypersensitive to TNF-alpha and showed reduced NF-kappaB function. Lithium treatment (which inhibits GSK-3; refs 8, 9) sensitized wild-type fibroblasts to TNF and inhibited transactivation of NF-kappaB. The early steps leading to NF-kappaB activation (degradation of I-kappaB and translocation of NF-kappaB to the nucleus) were unaffected by the loss of GSK-3beta, indicating that NF-kappaB is regulated by GSK-3beta at the level of the transcriptional complex. Thus, GSK-3beta facilitates NF-kappaB function.
糖原合酶激酶-3(GSK-3)α和β是密切相关的蛋白丝氨酸激酶,在胚胎发育以及成体组织细胞增殖过程中作为Wnt信号通路的抑制成分发挥作用。对GSK-3生理功能的深入了解源于在果蝇、盘基网柄菌和酵母中的遗传学分析。我们在此表明,小鼠GSK-3β基因的破坏导致胚胎致死,这是由妊娠中期严重肝变性引起的,该表型与过度的肿瘤坏死因子(TNF)毒性一致,正如在缺乏参与转录因子激活NF-κB激活相关基因的小鼠中所观察到的那样。使用抗TNF-α抗体抑制TNF可挽救GSK-3β缺陷胚胎。来自GSK-3β缺陷胚胎的成纤维细胞对TNF-α高度敏感,且显示出NF-κB功能降低。锂处理(抑制GSK-3;参考文献8、9)使野生型成纤维细胞对TNF敏感,并抑制NF-κB的反式激活。导致NF-κB激活的早期步骤(I-κB降解和NF-κB转位至细胞核)不受GSK-3β缺失的影响,这表明NF-κB在转录复合物水平受GSK-3β调节。因此,GSK-3β促进NF-κB功能。