雄激素受体激动剂与拮抗剂高通量筛选细胞模型的构建

发布时间：2018-06-09 17:12

本文选题：雄激素受体 + 激动剂　；参考：《基因组学与应用生物学》2015年03期

【摘要】：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。
[Abstract]:Effective androgen receptor AR-agonists and antagonists can up-regulate or down-regulate androgen receptor stimuli, and play a role in the treatment of related diseases. The establishment of high throughput cell screening model can enlarge the screening range of AR agonists and antagonists and accelerate the screening speed. In this study, recombinant human androgen receptor expression plasmid pcDNA3.1-h AR1 was constructed and co-transfected with MMTV-LTR-Luc F-R, a reporter gene plasmid regulated by androgen effector elements, into human embryonic renal cells 293T, and AR activation based on double luciferase reporter gene was constructed. Screening of high-throughput cell model. AR agonist 5 伪 -dihydrotestosterone could induce luciferase production in the cell model. Nilutamine, an AR antagonist, could antagonize the stimulation of 5 伪 -DHT. Dexamethasone, a glucocorticoid receptor agonist, has no effect on luciferase production in cell model.
【作者单位】：病原生物学与免疫学系广东药学院基础学院;索芙特(集团)有限公司研发中心;
【基金】：校企横向合作项目《育发类特殊用途化妆品中草药组方技术开发平台的构建》资助
【分类号】：R3416

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