In HepG2 cells overexpressing either AhR or Sp1, AhR determined the proximal transactivation of basal CYP1A1 expression. Via DNA affinity precipitation assays and ChIP, we found that AhR bound to the promoter and recruited Sp1 to transactivate CYP1A1 expression.

Jan 1, 2025 · Activating the AhR–CYP1A1 axis has emerged as a novel therapeutic strategy against various inflammatory diseases. Here, a practical in situ cell-based fluorometric assay was constructed to screen AhR-CYP1A1 axis modulators, via …

This review highlights the paucity of in vivo data on the effects of AHR antagonists and CYP1A1 inhibitors in rodent models of disease, namely the compound´s pharmacodynamics and tissue specificities for the mechanism of action; dose–effect dependence, AHR target genes, long term, and toxicity use.

In this review, we cover the state-of-the-art of the pharmacodynamic and pharmacokinetic properties of AHR antagonists and CYP1A1 inhibitors in different in vivo rodent (mouse or rat) models of disease.

The expression of CYP1A1 is transcriptionally up-regulated through the ligand-activated aryl hydrocarbon receptor (AhR). AhR plays an important role as mediator of an adaptive response to xenobiotics, as well as in normal physiology and embryonic development.

Nov 20, 2021 · This review highlights the paucity of in vivo data on the effects of AHR antagonists and CYP1A1 inhibitors in rodent models of disease, namely the compound´s pharmacodynamics and tissue specificities for the mechanism of action; dose–effect dependence, AHR target genes, long term, and toxicity use.

Jun 14, 2019 · Via DNA affinity precipitation assays and ChIP, we found that AhR bound to the promoter and recruited Sp1 to transactivate CYP1A1 expression. The coordinated interaction between Sp1 and AhR was identified to be DNA mediated.

The mammalian CYP1A1, CYP1A2, and CYP1B1 genes (encoding cytochromes P450 1A1, 1A2, and 1B1, respectively) are regulated by the aromatic hydrocarbon receptor (AHR). The CYP1 enzymes are responsible for both metabolically activating and detoxifying numerous polycyclic aromatic hydrocarbons (PAHs) and aromatic amines present in combustion products.

Apr 17, 2018 · Aryl hydrocarbon receptor (AhR) is a nuclear receptor that controls xenobiotic detoxification via induction of cytochrome P450 1A1 (CYP1A1) and regulates immune responses in the intestine....

1 day ago · Collectively, our findings reveal a novel link between ACP5 KO and the AHR-CYP1A1 inflammatory signaling pathway in DEP-exposed cells, and identify the AHR-CYP1A1 axis as a potential therapeutic ...