Cited by 489Toxic Organic Pollutants ImpactPharmacogenetics and Drug MetabolismCarcinogens and Genotoxicity Assessment

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Ligand binding and activation of the Ah receptor

Denison, Michael S, Pandini, Alessandro, Nagy, Scott R, Baldwin, Enoch P, Bonati, Laura·2002·Chemico-Biological Interactions

DOI 10.1016/s0009-2797(02)00063-7

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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.

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Authors: Denison, M. S., Pandini, A., Nagy, S. R., Baldwin, E. P., & Bonati, L.
Affiliations: University of California, Davis (US)
University of Milano-Bicocca (IT)
Corresponding author: Denison, Michael S
ORCID: Denison, Michael S
Pandini, Alessandro
Baldwin, Enoch P
Bonati, Laura
Venue: Chemico-Biological Interactions
Publisher: Elsevier BV
Published: 2002-09
Volume: 141
Issue: 1-2
Pages: 3-24
ISSN: 0009-2797 (ISSN-L)
DOI: 10.1016/s0009-2797(02)00063-7
OpenAlex: W1985754063
Cited by: 485
References: 153
Citations by year: 2026: 7 · 2025: 8 · 2024: 12 · 2023: 16 · 2022: 18 · 2021: 7 · 2020: 18 · 2019: 13 · 2018: 18 · 2017: 18 · 2016: 20 · 2015: 16 · 2014: 30 · 2013: 24 · 2012: 30
FWCI: 15.36
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Chemico-Biological Interactions (publishedVersion)
PubMed (publishedVersion)
BOA (University of Milano-Bicocca) (submittedVersion)
eScholarship (California Digital Library) (submittedVersion)
Funders: National Institutes of Health (5r01es007072-04)
National Institute of Environmental Health Sciences (ES07059, ES 07685, R01ES007685, ES-07072, ES5707, T32ES007059)
Topics: Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Toxic Organic Pollutants Impact
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Carcinogens and Genotoxicity Assessment
Keywords: aryl hydrocarbon receptor, ligand binding, receptor activation, ligand-binding domain, aromatic hydrocarbons, crystal structure, signal transduction, transcription factors
MeSH terms: Animals, Binding Sites, Humans, Ligands, Protein Binding, Protein Conformation, Signal Transduction, Receptors, Aryl Hydrocarbon

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Ligand binding and activation of the Ah receptor

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