Ligand binding and activation of the Ah receptor

Michael S. Denison, Alessandro Pandini, Scott R. Nagy, Enoch P. Baldwin, Laura Bonati

Research output: Contribution to journalArticle

335 Scopus citations

Abstract

The Ah receptor (AhR) is a ligand-dependent transcription factor that can be activated by structurally diverse synthetic and naturally-occurring chemicals. Although a significant amount of information is available with respect to the planar aromatic hydrocarbon AhR ligands, the actual spectrum of chemicals that can bind to and activate the AhR is only now being elucidated. In addition, the lack of information regarding the actual three-dimensional structure of the AhR ligand binding domain (LBD) has hindered detailed analysis of the molecular mechanisms by which these ligands bind to and active AhR signal transduction. In this review we describe the current state of knowledge with respect to naturally occurring AhR ligands and present and discuss the first theoretical model of the AhR LBD based on crystal structures of homologous PAS family members.

Original languageEnglish (US)
Pages (from-to)3-24
Number of pages22
JournalChemico-Biological Interactions
Volume141
Issue number1-2
DOIs
StatePublished - Sep 20 2002

Keywords

  • 2,3,7,8-Tetrachlorodibenzo-p-dioxin
  • Ah receptor
  • Dioxin
  • Homology model
  • Ligand binding domain
  • TCDD

ASJC Scopus subject areas

  • Toxicology

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    Denison, M. S., Pandini, A., Nagy, S. R., Baldwin, E. P., & Bonati, L. (2002). Ligand binding and activation of the Ah receptor. Chemico-Biological Interactions, 141(1-2), 3-24. https://doi.org/10.1016/S0009-2797(02)00063-7