Ganss R, Weih F, Schütz G
Division of Molecular Biology of the Cell I, German Cancer Research Center, Heidelberg.
Mol Endocrinol. 1994 Jul;8(7):895-903. doi: 10.1210/mend.8.7.7984151.
The pathway of gluconeogenesis is activated in liver shortly after birth and is controlled by glucagon and glucocorticoids, which stimulate, and insulin, which inhibits, the expression of genes coding for gluconeogenic enzymes. To understand the molecular basis of this cell type-specific and coordinate control, we analyzed the cis-regulatory elements of the tyrosine aminotransferase gene, which confer liver cell-specific expression in dependence of these hormones. The cAMP-responsive element (CRE) of the TAT gene is an essential element within a liver-specific enhancer and is recognized by the CRE-binding protein (CREB) in a phosphorylation-dependent manner. The glucocorticoid response is mediated by a complex regulatory unit comprised of the glucocorticoid receptor and other transcription factor-binding sites. Here, we show that both the cAMP- and glucocorticoid-inducible enhancers are targets for the antagonistic effects of insulin. The insulin-responsive sequences coincide with the CREB-binding site of the cAMP-responsive enhancer and a hepatocyte nuclear factor-3-binding site within the glucocorticoid-responsive unit. This design of the hormone-dependent enhancers reflects the molecular mechanism underlying the onset of tyrosine aminotransferase expression at birth when insulin levels decrease and concentrations of glucagon and glucocorticoids increase.
出生后不久,肝脏中的糖异生途径即被激活,该途径受胰高血糖素和糖皮质激素的刺激调控,同时也受胰岛素的抑制调控,胰岛素可抑制糖异生酶编码基因的表达。为了解这种细胞类型特异性和协同调控的分子基础,我们分析了酪氨酸转氨酶基因的顺式调控元件,这些元件可在这些激素的作用下赋予肝细胞特异性表达。TAT基因的cAMP反应元件(CRE)是肝脏特异性增强子中的一个关键元件,可被CRE结合蛋白(CREB)以磷酸化依赖的方式识别。糖皮质激素反应由一个由糖皮质激素受体和其他转录因子结合位点组成的复杂调控单元介导。在此,我们表明cAMP诱导型和糖皮质激素诱导型增强子均是胰岛素拮抗作用的靶点。胰岛素反应序列与cAMP反应增强子的CREB结合位点以及糖皮质激素反应单元内的肝细胞核因子-3结合位点一致。激素依赖性增强子的这种设计反映了出生时酪氨酸转氨酶表达开始的分子机制,此时胰岛素水平降低,胰高血糖素和糖皮质激素浓度升高。