Abstract
The Ah receptor (AhR) is a ligand-dependent transcription factor that call 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 an 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. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.
| Original language | English |
|---|---|
| Article number | PII S0009-2797(02)00063-7 |
| Pages (from-to) | 3-24 |
| Number of pages | 22 |
| Journal | Chemico-Biological Interactions |
| Volume | 141 |
| Issue number | 1-2 |
| Publication status | Published - 20 Sept 2002 |
Keywords
- Ah receptor
- 2,3,7,8-tetrachlorodibenzo-p-dioxin
- TCDD
- dioxin homology model
- ligand binding domain
- ARYL-HYDROCARBON RECEPTOR
- SIGNAL-TRANSDUCTION PATHWAY
- DIBENZO-P-DIOXINS
- POLYCHLORINATED-BIPHENYLS PCBS
- NUCLEAR TRANSLOCATOR PROTEIN
- HEAT-SHOCK PROTEIN
- ARACHIDONIC-ACID METABOLISM
- CYP1A1 GENE-EXPRESSION
- LIVER-CELL CULTURE
- HELIX-LOOP-HELIX