Tsai S Y, Srinivasan G, Allan G F, Thompson E B, O'Malley B W, Tsai M J
Department of Cell Biology, Baylor College of Medicine, Houston, Texas 77030.
J Biol Chem. 1990 Oct 5;265(28):17055-61.
A recombinant full length human glucocorticoid receptor stimulates transcription in vitro of test genes containing synthetic glucocorticoid and progesterone response elements or murine mammary tumor virus promoter. The receptor expressed in a baculoviral vector is highly active, enhancing transcription of hormone response genes greater than 30-fold even at a receptor concentration of 1.2 nM. The enhancement of transcription is glucocorticoid and progesterone response element-dependent, suggesting that it is a receptor mediated event. In vitro and in vivo treatment with the agonist dexamethasone or with the antagonist Ru486 did not alter significantly the functional activity of partially purified receptor. Kinetic studies suggest that both glucocorticoid receptor and HeLa cell extracts are required for formation of a stable committed transcriptional complex. Our results indicate that the action of glucocorticoid receptor on gene transcription is similar to that defined recently for the progesterone receptor and may be a general mechanism for all steroid receptors.
一种重组全长人糖皮质激素受体在体外刺激含有合成糖皮质激素和孕酮反应元件或小鼠乳腺肿瘤病毒启动子的测试基因的转录。在杆状病毒载体中表达的该受体具有高活性，即使在受体浓度为1.2 nM时，也能将激素反应基因的转录增强30倍以上。转录增强依赖于糖皮质激素和孕酮反应元件，表明这是一个受体介导的事件。用激动剂地塞米松或拮抗剂米非司酮进行体外和体内处理，并未显著改变部分纯化受体的功能活性。动力学研究表明，形成稳定的转录起始复合物需要糖皮质激素受体和HeLa细胞提取物。我们的结果表明，糖皮质激素受体对基因转录的作用与最近定义的孕酮受体的作用相似，可能是所有类固醇受体的普遍机制。
