Mihelakis Melina, Flore Tanina, Schönfelder Gilbert, Oelgeschläger Michael, Ertych Norman
German Centre for the Protection of Laboratory Animals (Bf3R), German Federal Institute for Risk Assessment, Diedersdorfer Weg 1, 12277, Berlin, Germany.
Department of Clinical Pharmacology and Toxicology, Charité - Universitätsmedizin Berlin, Berlin, Germany.
Cell Biol Toxicol. 2025 Sep 12;41(1):130. doi: 10.1007/s10565-025-10080-0.
The Aryl Hydrocarbon Receptor (AHR) is a crucial mediator of cellular responses upon exposure to environmental pollutants. Initially described as central activator in xenobiotic metabolism, recent research has unveiled additional layers of complexity in AHR function and regulation. The circadian rhythm is a fundamental regulatory process that modulates various physiological processes, including AHR activity. Our recent findings show that AHR-dependent gene induction is subject to circadian rhythmicity. While some studies suggest a circadian AHR gene transcription in various tissues, a comprehensive mechanistic understanding of the circadian AHR regulation remains elusive. This mechanistic study aimed to elucidate the circadian regulation of AHR target gene induction upon dioxin treatment in human breast cells. To acquire a more profound understanding of the intricacies of AHR regulation, we conducted a systematic analysis of the molecular co-factors and their interactions in circadian synchronized cells. Our results show circadian regulation of AHR transcriptional activity at the CYP1A1 promoter upon dioxin treatment. This appears to be orchestrated by the core clock components BMAL1/CLOCK, which directly interact with AHR in circadian synchronized cells. Additionally, we identified SP1 as an important positive and p23 as an essential negative regulator of circadian AHR activity. The understanding of these interactions is crucial for elucidating the molecular relationship between the circadian clock and cellular responses to environmental stimuli. Such knowledge is of vital importance for the application of New Approach Methods (NAMs) as part of a weight-of-evidence (WoE) approach in the next generation of risk assessments.
芳烃受体(AHR)是细胞暴露于环境污染物后细胞反应的关键介质。最初被描述为异生物质代谢的核心激活剂,最近的研究揭示了AHR功能和调控的更多复杂层面。昼夜节律是一种基本的调节过程,可调节包括AHR活性在内的各种生理过程。我们最近的研究结果表明,AHR依赖性基因诱导受昼夜节律影响。虽然一些研究表明在各种组织中存在昼夜节律性的AHR基因转录,但对昼夜节律性AHR调控的全面机制理解仍然难以捉摸。这项机制研究旨在阐明二噁英处理后人乳腺细胞中AHR靶基因诱导的昼夜节律调控。为了更深入地了解AHR调控的复杂性,我们对昼夜节律同步细胞中的分子辅助因子及其相互作用进行了系统分析。我们的结果表明,二噁英处理后,CYP1A1启动子处的AHR转录活性存在昼夜节律调控。这似乎是由核心生物钟组件BMAL1/CLOCK协调的,它们在昼夜节律同步细胞中直接与AHR相互作用。此外,我们确定SP1是昼夜节律性AHR活性的重要正调节因子,而p23是必不可少的负调节因子。理解这些相互作用对于阐明生物钟与细胞对环境刺激反应之间的分子关系至关重要。这些知识对于作为下一代风险评估中证据权重(WoE)方法一部分的新方法(NAMs)的应用至关重要。