title: Ligand binding and activation of the Ah receptor.
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.
authors.affiliation: Department of Environmental Toxicology, Meyer Hall, One Shields Avenue, University of California, Davis 95616-8588, USA. msdenison@ucdavis.edu
authors.forename: Michael S
authors.initials: MS
authors.lastname: Denison
authors.forename: Alessandro
authors.initials: A
authors.lastname: Pandini
authors.forename: Scott R
authors.initials: SR
authors.lastname: Nagy
authors.forename: Enoch P
authors.initials: EP
authors.lastname: Baldwin
authors.forename: Laura
authors.initials: L
authors.lastname: Bonati
mesh_terms: D000818:Animals; D001665:Binding Sites; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D011487:Protein Conformation; D018336:Receptors, Aryl Hydrocarbon / Q000819:agonists* / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D008024:Ligands; D018336:Receptors, Aryl Hydrocarbon