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

Michael S. Denison, Scott R. Nagy

Research output: Contribution to journalArticlepeer-review

1248 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)309-334
Number of pages26
JournalAnnual Review of Pharmacology and Toxicology
Volume43
DOIs
StatePublished - 2003

Keywords

  • 2,3,7,8-Tetrachlorodibenzo-p-dioxin
  • Ah receptor
  • Ah receptor ligands
  • CYP1A1
  • TCDD

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

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