Doble Bradley W, Woodgett James R
Samuel Lunenfeld Research Institute, Toronto, Ont., Canada.
Cells Tissues Organs. 2007;185(1-3):73-84. doi: 10.1159/000101306.
Epithelial cells usually exist as sheets of immotile, tightly packed, well-coupled, polarized cells with distinct apical, basal and lateral surfaces. Remarkably, these cells can dramatically alter their morphology to become motile, fibroblast-like mesenchymal cells in a process of epithelial-mesenchymal transition (EMT). This process and the reverse, mesenchymal-epithelial transition, occur repeatedly during normal embryonic development. A phenomenon similar to physiological EMT occurs during the pathophysiological progression of some cancers. Tumours of epithelial origin, as they transform to malignancy, appear to exploit the innate plasticity of epithelial cells, with EMT conferring increased invasiveness and metastatic potential. Key to the maintenance of epithelial cell identity is the expression of E-cadherin, a protein that is required for tight intercellular adhesion along the lateral surfaces of adjacent epithelial cells. Loss of functional E-cadherin is a critical event in EMT. An important regulator of E-cadherin expression is the protein Snail, a zinc-finger transcriptional repressor. Snail contains several consensus sites for the kinase, glycogen synthase kinase-3 (GSK-3), and accumulating evidence indicates that it is a GSK-3 substrate. Phosphorylation of Snail by GSK-3 facilitates its proteasomal degradation. Conversely, inhibition of GSK-3 leads to Snail accumulation, E-cadherin downregulation, and development of EMT in cultured epithelial cells. Several signalling pathways implicated in the progression of EMT, including the Wnt and phosphoinositide 3-kinase pathways, use GSK-3 to mediate their responses. In these pathways, GSK-3's regulation of other transcriptional effectors like beta-catenin works in concert with changes in Snail to orchestrate the EMT process. This review focuses on the emerging role of GSK-3 as a modulator of cell fate and EMT in the contexts of development, in vitro cell culture and cancer.
上皮细胞通常以片状形式存在,这些细胞不能移动、紧密排列、连接良好且呈极化状态,具有明显的顶端、基底和侧面。值得注意的是,在上皮-间质转化(EMT)过程中,这些细胞可显著改变其形态,变成可移动的、成纤维细胞样的间充质细胞。这个过程以及相反的间质-上皮转化,在正常胚胎发育过程中会反复发生。在某些癌症的病理生理进展过程中,会出现类似于生理性EMT的现象。起源于上皮的肿瘤在转变为恶性肿瘤时,似乎利用了上皮细胞固有的可塑性,EMT赋予肿瘤细胞更强的侵袭性和转移潜能。维持上皮细胞特性的关键是E-钙黏蛋白的表达,这种蛋白质是相邻上皮细胞侧面紧密细胞间黏附所必需的。功能性E-钙黏蛋白的缺失是EMT中的一个关键事件。E-钙黏蛋白表达的一个重要调节因子是Snail蛋白,它是一种锌指转录抑制因子。Snail含有激酶糖原合酶激酶-3(GSK-3)的几个共有位点,越来越多的证据表明它是GSK-3的底物。GSK-3对Snail的磷酸化促进其通过蛋白酶体降解。相反,抑制GSK-3会导致Snail积累、E-钙黏蛋白下调,并在培养的上皮细胞中引发EMT。与EMT进展相关的几种信号通路,包括Wnt和磷酸肌醇3-激酶通路,利用GSK-3来介导它们的反应。在这些通路中,GSK-3对其他转录效应因子(如β-连环蛋白)的调节与Snail的变化协同作用,共同调控EMT过程。本综述重点关注GSK-3在发育、体外细胞培养和癌症背景下作为细胞命运和EMT调节因子的新作用。