Institute of Cellular Biology and Pathology, Nicolae Simionescu of the Romanian Academy, Bucharest, Romania.
PLoS One. 2012;7(7):e40463. doi: 10.1371/journal.pone.0040463. Epub 2012 Jul 12.
Apolipoprotein CII (apoCII) is a specific activator of lipoprotein lipase and plays an important role in triglyceride metabolism. The aim of our work was to elucidate the regulatory mechanisms involved in apoCII gene modulation in macrophages. Using Chromosome Conformation Capture we demonstrated that multienhancer 2 (ME.2) physically interacts with the apoCII promoter and this interaction facilitates the transcriptional enhancement of the apoCII promoter by the transcription factors bound on ME.2. We revealed that the transcription factor STAT1, previously shown to bind to its specific site on ME.2, is functional for apoCII gene upregulation. We found that siRNA-mediated inhibition of STAT1 gene expression significantly decreased the apoCII levels, while STAT1 overexpression in RAW 264.7 macrophages increased apoCII gene expression. Using transient transfections, DNA pull down and chromatin immunoprecipitation assays, we revealed a novel STAT1 binding site in the -500/-493 region of the apoCII promoter, which mediates apoCII promoter upregulation by STAT1. Interestingly, STAT1 could not exert its upregulatory effect when the RXRα/T3Rβ binding site located on the apoCII promoter was mutated, suggesting physical and functional interactions between these factors. Using GST pull-down and co-immunoprecipitation assays, we demonstrated that STAT1 physically interacts with RXRα. Taken together, these data revealed that STAT1 bound on ME.2 cooperates with RXRα located on apoCII promoter and upregulates apoCII expression only in macrophages, due to the specificity of the long-range interactions between the proximal and distal regulatory elements. Moreover, we showed for the first time that STAT1 and RXRα physically interact to exert their regulatory function.
载脂蛋白 CII(apoCII)是脂蛋白脂肪酶的特异性激活剂,在甘油三酯代谢中发挥重要作用。我们的工作旨在阐明调节巨噬细胞中 apoCII 基因表达的调控机制。使用染色质构象捕获技术,我们证明多增强子 2(ME.2)与 apoCII 启动子物理相互作用,这种相互作用促进了结合在 ME.2 上的转录因子对 apoCII 启动子的转录增强。我们揭示了先前显示与 ME.2 上其特定位点结合的转录因子 STAT1 是 apoCII 基因上调的功能。我们发现,siRNA 介导的 STAT1 基因表达抑制显著降低了 apoCII 水平,而 RAW 264.7 巨噬细胞中 STAT1 的过表达增加了 apoCII 基因的表达。通过瞬时转染、DNA 拉下和染色质免疫沉淀测定,我们在 apoCII 启动子的-500/-493 区域发现了一个新的 STAT1 结合位点,该位点介导了 STAT1 对 apoCII 启动子的上调。有趣的是,当位于 apoCII 启动子上的 RXRα/T3Rβ 结合位点发生突变时,STAT1 无法发挥其上调作用,这表明这些因子之间存在物理和功能相互作用。通过 GST 拉下和共免疫沉淀测定,我们证明 STAT1 与 RXRα 物理相互作用。总之,这些数据表明,结合在 ME.2 上的 STAT1 与位于 apoCII 启动子上的 RXRα 相互作用,并仅在巨噬细胞中上调 apoCII 表达,这归因于近端和远端调节元件之间的长程相互作用的特异性。此外,我们首次表明 STAT1 和 RXRα 物理相互作用以发挥其调节功能。