Binding characterization, synthesis and biological evaluation of RXRα antagonists targeting the coactivator binding site

Bioorganic & Medicinal Chemistry Letters(2016)

引用 6|浏览11
暂无评分
摘要
Previously we identified the first retinoid X receptor-alpha (RXRα) modulators that regulate the RXRα biological function via binding to the coregulator-binding site. Here we report the characterization of the interactions between the hit molecule and RXRα through computational modeling, mutagenesis, SAR and biological evaluation. In addition, we reported studies of additional new compounds and identified a molecule that mediated the NF-κB pathway by inhibiting the TNFα-induced IκBα degradation and p65 nuclear translocation.
更多
查看译文
关键词
Nuclear receptors,RXRα modulators,Coregulator-binding site,Coactivator-binding site ligand,TNFα/NF-κB pathway
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要