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Activation of the Aryl Hydrocarbon Receptor by Structurally Diverse Exogenous and Endogenous Chemicals

2003/01/22 by Michael S. Denison, Scott R. Nagy
Environmental Science · Medicine · #Adipose Tissue and Metabolism #Effects and risks of endocrine disrupting chemicals #Toxic Organic Pollutants Impact

paper · doi:10.1146/annurev.pharmtox.43.100901.135828

openalex publication_date 2003/01/22 · openalex created_date 2025/10/10 · openalex updated_date 2026/08/01

Abstract

The induction of expression of genes for xenobiotic metabolizing enzymes in response to chemical insult is an adaptive response found in most organisms. In vertebrates, the AhR is one of several chemical/ligand-dependent intracellular receptors that can stimulate gene transcription in response to xenobiotics. The ability of the AhR to bind and be activated by a range of structurally divergent chemicals suggests that the AhR contains a rather promiscuous ligand binding site. In addition to synthetic and environmental chemicals, numerous naturally occurring dietary and endogenous AhR ligands have also been identified. In this review, we describe evidence for the structural promiscuity of AhR ligand binding and discuss the current state of knowledge with regards to the activation of the AhR signaling pathway by naturally occurring exogenous and endogenous ligands.

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