Giguère V, Hollenberg S M, Rosenfeld M G, Evans R M
Cell. 1986 Aug 29;46(5):645-52. doi: 10.1016/0092-8674(86)90339-9.
Human glucocorticoid receptor (hGR) produced in CV-1 cells via transfection of an hGR expression vector functions as a necessary and sufficient factor for the transcriptional activation of the MTV-CAT fusion gene. The magnitude of the induction (500-1000 fold) reveals that the hGR may act as a transcriptional "switch," converting a silent promoter containing a glucocorticoid response element to an activated state. Stimulation of transcription of the MTV-CAT gene fusion by hGR is not dependent on transcriptional factors that are limiting in CV-1 cells. Characterization of 27 insertional mutants of the hGR allowed the location of at least four functional domains, two of which correspond to the predicted DNA- and steroid-binding domains. The other two domains are referred to as tau (tau) for their potent effects on transcription. This raises the possibility that other regions in the receptor are necessary for full transcriptional activation but are not specifically involved in steroid or DNA binding.
通过转染人糖皮质激素受体（hGR）表达载体在CV - 1细胞中产生的hGR，作为MTV - CAT融合基因转录激活的必要且充分因子发挥作用。诱导幅度（500 - 1000倍）表明hGR可能作为转录“开关”，将含有糖皮质激素反应元件的沉默启动子转变为激活状态。hGR对MTV - CAT基因融合转录的刺激不依赖于CV - 1细胞中有限的转录因子。对hGR的27个插入突变体的表征确定了至少四个功能域，其中两个对应于预测的DNA和类固醇结合域。另外两个域因其对转录的强大作用而被称为tau（τ）。这增加了一种可能性，即受体中的其他区域对于完全转录激活是必需的，但不专门参与类固醇或DNA结合。
