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有效的雄激素受体(androgen receptor,AR)激动剂与拮抗剂,可上调或下调雄激素受体刺激反应,起到治疗相关疾病的作用。高通量细胞筛选模型的建立,可扩大AR激动剂与拮抗剂筛选范围,加快筛选速度。本研究通过构建人雄激素受体表达重组质粒pcDNA 3.1-h AR,并与受雄激素效应元件调控的报告基因质粒MMTV-LTR-Luc F-R共转染人胚胎肾细胞293T,构建基于双荧光素酶报告基因的AR激动剂与拮抗剂筛选高通量细胞模型。AR激动剂5α-双氢睾酮可诱导该细胞模型荧光素酶的产生,AR拮抗剂尼鲁他明可拮抗5α-DHT的刺激作用,糖皮质激素受体激动剂地塞米松对细胞模型荧光素酶的产生无作用。
Effective androgen receptor (AR) agonists and antagonists can upregulate or downregulate the androgen receptor stimulating response and play a role in the treatment of related diseases. The establishment of a high-throughput cell selection model can expand the scope of AR agonist and antagonist screening and speed up screening. In this study, recombinant human pcDNA 3.1-h AR was constructed by human androgen receptor and transfected into human embryonic kidney 293T cells with reporter gene plasmid MMTV-LTR-Luc FR regulated by androgen-responsive elements. AR reporter and antagonist screening of high-throughput cell models. The AR agonist 5α-dihydrotestosterone induced luciferase production in this cell model. The AR antagonist Nalutatamine antagonized the stimulation of 5α-DHT. The dexamethasone, a glucocorticoid receptor agonist, No effect of enzyme production.