Onuma Hiroshi, Oeser James K, Nelson Bryce A, Wang Yingda, Flemming Brian P, Scheving Lawrence A, Russell William E, O'Brien Richard M
Department of Molecular Physiology and Biophysics, Vanderbilt University Medical School, Nashville, TN 37232, U.S.A.
Biochem J. 2009 Jan 15;417(2):611-20. doi: 10.1042/BJ20080999.
The G6Pase (glucose-6-phosphatase catalytic subunit) catalyses the final step in the gluconeogenic and glycogenolytic pathways, the hydrolysis of glucose-6-phosphate to glucose. We show here that, in HepG2 hepatoma cells, EGF (epidermal growth factor) inhibits basal mouse G6Pase fusion gene transcription. Several studies have shown that insulin represses basal mouse G6Pase fusion gene transcription through FOXO1 (forkhead box O1), but Stoffel and colleagues have recently suggested that insulin can also regulate gene transcription through FOXA2 (forkhead box A2) [Wolfrum, Asilmaz, Luca, Friedman and Stoffel (2003) Proc. Natl. Acad. Sci. 100, 11624-11629]. A combined GR (glucocorticoid receptor)-FOXA2 binding site is located between -185 and -174 in the mouse G6Pase promoter overlapping two FOXO1 binding sites located between (-188 and -182) and (-174 and -168). Selective mutation of the FOXO1 binding sites reduced the effect of insulin, whereas mutation of the GR/FOXA2 binding site had no effect on the insulin response. In contrast, selective mutation of the FOXO1 and GR/FOXA2 binding sites both reduced the effect of EGF. The effect of these mutations was additive, since the combined mutation of both FOXO1 and GR/FOXA2 binding sites reduced the effect of EGF to a greater extent than the individual mutations. These results suggest that, in HepG2 cells, GR and/or FOXA2 are required for the inhibition of basal G6Pase gene transcription by EGF but not insulin. EGF also inhibits hepatic G6Pase gene expression in vivo, but in cultured hepatocytes EGF has the opposite effect of stimulating expression, an observation that may be explained by a switch in ErbB receptor sub-type expression following hepatocyte isolation.
葡萄糖-6-磷酸酶催化亚基(G6Pase)催化糖异生和糖原分解途径的最后一步,即将葡萄糖-6-磷酸水解为葡萄糖。我们在此表明,在HepG2肝癌细胞中,表皮生长因子(EGF)抑制基础小鼠G6Pase融合基因转录。多项研究表明,胰岛素通过叉头框O1(FOXO1)抑制基础小鼠G6Pase融合基因转录,但施托费尔及其同事最近提出,胰岛素也可通过叉头框A2(FOXA2)调节基因转录[沃尔弗鲁姆、阿斯尔马兹、卢卡、弗里德曼和施托费尔(2003年)《美国国家科学院院刊》100, 11624 - 11629]。在小鼠G6Pase启动子中,一个糖皮质激素受体(GR)-FOXA2结合位点组合位于-185至-174之间,与位于(-188至-182)和(-174至-168)之间的两个FOXO1结合位点重叠。FOXO1结合位点的选择性突变降低了胰岛素的作用,而GR/FOXA2结合位点的突变对胰岛素反应没有影响。相反,FOXO1和GR/FOXA2结合位点的选择性突变均降低了EGF的作用。这些突变的作用是累加的,因为FOXO1和GR/FOXA2结合位点的联合突变比单个突变更显著地降低了EGF的作用。这些结果表明,在HepG2细胞中,GR和/或FOXA2是EGF而非胰岛素抑制基础G6Pase基因转录所必需的。EGF在体内也抑制肝脏G6Pase基因表达,但在培养的肝细胞中,EGF具有刺激表达的相反作用这一现象,可能可通过肝细胞分离后ErbB受体亚型表达的转变来解释。