Simon Marie-Pierre, Tournaire Roselyne, Pouyssegur Jacques
Institute of Signaling, Developmental Biology and Cancer Research, CNRS UMR 6543, University of Nice, Centre A. Lacassagne, Nice, France.
J Cell Physiol. 2008 Dec;217(3):809-18. doi: 10.1002/jcp.21558.
Angiopoietins are ligands of the endothelial cell tyrosine kinase receptor Tie2. Angiopoietin-1 (Ang-1) is widely expressed in human normal adult tissues and promotes blood vessel maturation and stabilization by inducing Tie2 receptor phosphorylation. In contrast, the antagonistic ligand Angiopoietin-2 (Ang-2) is up-regulated by hypoxia, expressed only at sites of vascular remodeling and plays a crucial role in destabilizing vessels for normal or pathological angiogenesis. Ang-2 expression is tightly regulated at transcriptional and post-transcriptional levels. To characterize the regulatory sequences of the human Ang-2 gene we cloned a fragment of around 8.5 kb upstream of the Ang-2 coding sequence and analyzed the luciferase reporter activity of constructs of various lengths in endothelial and non-endothelial cells. We isolated a minimal promoter sequence sufficient to promote significant Ang-2 non-cell type specific transcription. Moreover, we identified sequences conferring endothelial specificity. Indeed, sequence analysis of the fragment revealed the presence of several potential binding sites for specific endothelial regulatory factors like GATA or Ets. Using GATA-2 and Ets-1 co-transfection and overexpression assay, we showed that these two factors are able to induce Ang-2 promoter activation. We also show that hypoxic regulation of Ang-2 is HIF-dependent and demonstrate that HIF-1alpha binds in human microvascular endothelial cells (HMVEC) to an evolutionary conserved Hypoxia-Responsive Element (HRE) located in the first intron of the Ang-2 gene. In conclusion, our study provides new elements in favor of HIF involvement in Ang-2 hypoxic regulation and identifies Ets-1 and particularly GATA-2 as central factors in endothelial specific Ang-2 expression.
血管生成素是内皮细胞酪氨酸激酶受体Tie2的配体。血管生成素-1(Ang-1)在人类正常成人组织中广泛表达,并通过诱导Tie2受体磷酸化促进血管成熟和稳定。相比之下,拮抗性配体血管生成素-2(Ang-2)在缺氧状态下上调,仅在血管重塑部位表达,并且在正常或病理性血管生成过程中使血管不稳定方面发挥关键作用。Ang-2的表达在转录和转录后水平受到严格调控。为了表征人类Ang-2基因的调控序列,我们克隆了Ang-2编码序列上游约8.5 kb的片段,并分析了不同长度构建体在内皮细胞和非内皮细胞中的荧光素酶报告基因活性。我们分离出了一个足以促进显著的Ang-2非细胞类型特异性转录的最小启动子序列。此外,我们鉴定出了赋予内皮细胞特异性的序列。实际上,对该片段的序列分析揭示了存在几个特定内皮细胞调节因子(如GATA或Ets)的潜在结合位点。通过GATA-2和Ets-1共转染及过表达实验,我们表明这两个因子能够诱导Ang-2启动子激活。我们还表明Ang-2的缺氧调节是HIF依赖性的,并证明HIF-1α在人微血管内皮细胞(HMVEC)中与位于Ang-2基因第一内含子中的进化保守缺氧反应元件(HRE)结合。总之,我们的研究提供了有利于HIF参与Ang-2缺氧调节的新证据,并确定Ets-1,特别是GATA-2是内皮细胞特异性Ang-2表达的核心因子。