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Regulation of Aryl Hydrocarbon Receptor Signaling Pathway and Dioxin Toxicity by Novel Agonists and Antagonists.
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-01-09 , DOI: 10.1021/acs.chemrestox.9b00431 Yin Liu 1, 2 , Yongyi Wei 3, 4 , Songyan Zhang 1, 2 , Xiliang Yan 4, 5 , Hao Zhu 5 , Li Xu 1, 2 , Bin Zhao 1, 2 , Heidi Qunhui Xie 1, 2 , Bing Yan 3, 4
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-01-09 , DOI: 10.1021/acs.chemrestox.9b00431 Yin Liu 1, 2 , Yongyi Wei 3, 4 , Songyan Zhang 1, 2 , Xiliang Yan 4, 5 , Hao Zhu 5 , Li Xu 1, 2 , Bin Zhao 1, 2 , Heidi Qunhui Xie 1, 2 , Bing Yan 3, 4
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Dioxins, mostly through activation of aryl hydrocarbon receptor (AhR), are potent toxic substances widely distributed in the environment, while moderated suppression of AhR also exhibits anti-tumor effects. Therefore, the proper modulation of AhR activity may counteract AhR-mediated toxicities and certain diseases. In this investigation, we identified several novel AhR moderate agonists and antagonists using chemical biology approaches. The mechanisms and mode of interactions with AhR by these hits were also revealed using both experimental and computational studies. The newly identified AhR moderate agonists and antagonists were predicted to bind to AhR and modulate AhR signaling. The structure-activity relationships of moderate agonists and antagonists and their unique binding features with AhR have created a solid framework for further optimization of the next generation of AhR modulators.
中文翻译：
新型激动剂和拮抗剂调节芳烃受体信号通路和二恶英毒性。
二恶英主要通过活化芳烃受体（AhR）来活化，是在环境中广泛分布的有效有毒物质，而适度抑制AhR也表现出抗肿瘤作用。因此，适当调节AhR活性可以抵消AhR介导的毒性和某些疾病。在这项调查中，我们使用化学生物学方法鉴定了几种新型的AhR中度激动剂和拮抗剂。还通过实验和计算研究揭示了这些命中与AhR相互作用的机制和方式。预测新鉴定的AhR中度激动剂和拮抗剂与AhR结合并调节AhR信号传导。
更新日期：2020-01-09
中文翻译：
新型激动剂和拮抗剂调节芳烃受体信号通路和二恶英毒性。
二恶英主要通过活化芳烃受体（AhR）来活化，是在环境中广泛分布的有效有毒物质，而适度抑制AhR也表现出抗肿瘤作用。因此，适当调节AhR活性可以抵消AhR介导的毒性和某些疾病。在这项调查中，我们使用化学生物学方法鉴定了几种新型的AhR中度激动剂和拮抗剂。还通过实验和计算研究揭示了这些命中与AhR相互作用的机制和方式。预测新鉴定的AhR中度激动剂和拮抗剂与AhR结合并调节AhR信号传导。
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