3 条结果 关键词:雄激素受体 ×

High-Content Screening Campaign to Identify Compounds That Inhibit or Disrupt Androgen Receptor-Transcriptional Intermediary Factor 2 Protein-Protein Interactions for the Treatment of Prostate Cancer.

Assay and drug development technologies 2018 Fancher AT, Hua Y, Camarco DP, Close DA 等 6 人

约20%前列腺癌(PCa)患者会进展为不可治愈的去势抵抗性前列腺癌(CRPC),雄激素受体(AR)共激活因子转录中介因子2(TIF2)过表达与不良预后相关。本研究将AR-TIF2蛋白-蛋白相互作用生物传感器(PPIB)高内容筛选(HCS)应用于143,535个化合物,筛选能抑制双氢睾酮(DHT)诱导的AR-TIF2相互作用形成或破坏...

High Content Positional Biosensor Assay to Screen for Compounds that Prevent or Disrupt Androgen Receptor and Transcription Intermediary Factor 2 Protein-Protein Interactions.

Methods in molecular biology (Clifton, N.J.) 2018 Hua Y, Camarco DP, Strock CJ, Johnston PA

转录中介因子2(TIF2)是雄激素受体(AR)的关键共激活因子,参与去势抵抗性前列腺癌(CRPC)的发生与进展。本章报道了一种AR-TIF2蛋白-蛋白相互作用(PPI)生物传感器检测,用于筛选能够诱导AR-TIF2 PPI、抑制二氢睾酮(DHT)诱导的AR-TIF2 PPI形成或破坏已有AR-TIF2 PPI的小分子。该检测采用高内...

High-content positional biosensor screening assay for compounds to prevent or disrupt androgen receptor and transcriptional intermediary factor 2 protein-protein interactions.

Assay and drug development technologies 2014 Hua Y, Shun TY, Strock CJ, Johnston PA

本文报道了一种用于筛选可预防或破坏雄激素受体(AR)与转录中介因子2(TIF2)蛋白-蛋白相互作用(PPI)的高内容定位生物传感器检测法。重组腺病毒分别表达融合红色荧光蛋白(RFP)的AR配体结合域/激活功能2表面域(含核定位与核输出序列)和融合绿色荧光蛋白(GFP)的TIF2三个LXXLL基序(含HIV Rev核仁定位序列)。未刺...