Department of Life Science, University of Seoul, Siripdae-gil 13, Dongdaemun-gu, Seoul 130-743, Republic of Korea.
J Biol Chem. 2010 Jan 29;285(5):3289-99. doi: 10.1074/jbc.M109.059212. Epub 2009 Nov 25.
Upon exposure to adipogenesis-inducing hormones, confluent 3T3-L1 preadipocytes express C/EBPbeta (CCAAT/enhancer binding protein beta). Early induced C/EBPbeta is inactive but, after a lag period, acquires its DNA-binding capability by sequential phosphorylation. During this period, preadipocytes pass the G(1)/S checkpoint synchronously. Thr(188) of C/EBPbeta is phosphorylated initially to prime the factor for subsequent phosphorylation at Ser(184) or Thr(179) by GSK3beta, which translocates into the nuclei during the G(1)/S transition. Many events take place during the G(1)/S transition, including reduction in p27(Kip1) protein levels, retinoblastoma (Rb) phosphorylation, GSK3beta nuclear translocation, and C/EBPbeta binding to target promoters. During hypoxia, hypoxia-inducible factor-1alpha (HIF-1alpha) is stabilized, thus maintaining expression of p27(Kip1), which inhibits Rb phosphorylation. Even under normoxic conditions, constitutive expression of p27(Kip1) blocks the nuclear translocation of GSK3beta and DNA binding capability of C/EBPbeta. Hypoxia also blocks nuclear translocation of GSK3beta and DNA binding capability of C/EBPbeta in HIF-1alpha knockdown 3T3-L1 cells that fail to induce p27(Kip1). Nonetheless, under hypoxia, these cells can block Rb phosphorylation and the G(1)/S transition. Altogether, these findings suggest that hypoxia prevents the nuclear translocation of GSK3beta and the DNA binding capability of C/EBPbeta by blocking the G(1)/S transition through HIF-1alpha-dependent induction of p27(Kip1) and an HIF-1alpha/p27-independent mechanism.
在接触到诱导脂肪生成的激素后,融合的 3T3-L1 前脂肪细胞表达 C/EBPβ(CCAAT/增强子结合蛋白β)。早期诱导的 C/EBPβ是无活性的,但在延迟期后,通过顺序磷酸化获得其 DNA 结合能力。在此期间,前脂肪细胞同步通过 G1/S 检查点。C/EBPβ 的 Thr188 首先被磷酸化,为随后由 GSK3β 在 Ser184 或 Thr179 进行的磷酸化做好准备,GSK3β 在 G1/S 转换期间转位到核内。在 G1/S 转换期间发生了许多事件,包括 p27(Kip1)蛋白水平降低、视网膜母细胞瘤(Rb)磷酸化、GSK3β 核转位以及 C/EBPβ 与靶启动子结合。在缺氧条件下,缺氧诱导因子-1α(HIF-1α)被稳定,从而维持 p27(Kip1)的表达,抑制 Rb 磷酸化。即使在常氧条件下,p27(Kip1)的组成性表达也会阻止 GSK3β 的核转位和 C/EBPβ 的 DNA 结合能力。缺氧还会阻止 HIF-1α 敲低的 3T3-L1 细胞中的 GSK3β 核转位和 C/EBPβ 的 DNA 结合能力,这些细胞无法诱导 p27(Kip1)。然而,在缺氧条件下,这些细胞可以阻止 Rb 磷酸化和 G1/S 转换。总之,这些发现表明,缺氧通过 HIF-1α 依赖性诱导 p27(Kip1)和 HIF-1α/p27 非依赖性机制阻止 G1/S 转换,从而阻止 GSK3β 的核转位和 C/EBPβ 的 DNA 结合能力。