Target type: cellularcomponent
An aryl hydrocarbon receptor complex found in the cytosol, in which the ligand-binding subunit AhR is not bound to ligand; consists of AhR, two molecules of HSP90, the protein kinase c-Src, and the immunophilin XAP2/AIP. [PMID:7598497, PMID:8937476, PMID:9447995]
The cytosolic aryl hydrocarbon receptor (AhR) complex is a multi-protein assembly that serves as a crucial sensor for environmental toxins and other xenobiotics. The core of the complex consists of the AhR protein, which is a ligand-activated transcription factor, along with the heat shock protein 90 (Hsp90) chaperone and the co-chaperone AIP (aryl hydrocarbon receptor interacting protein). This complex resides in the cytoplasm, maintaining the AhR in an inactive state. Upon encountering a ligand, such as dioxins or polycyclic aromatic hydrocarbons, the AhR undergoes a conformational change, leading to the release of Hsp90 and AIP. This allows the AhR to translocate to the nucleus where it dimerizes with the aryl hydrocarbon receptor nuclear translocator (ARNT). This dimer binds to specific DNA sequences known as dioxin-responsive elements (DREs) in the promoter region of target genes, thereby initiating their transcription. The cytosolic AhR complex is a dynamic entity, with the composition and interactions of its constituent proteins subject to modulation by various cellular factors, including the presence of specific ligands, post-translational modifications, and the availability of interacting partners. This dynamic nature allows the AhR to finely tune its responsiveness to environmental stimuli, ensuring appropriate cellular responses to xenobiotics.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Aryl hydrocarbon receptor | An aryl hydrocarbon receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P35869] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| dibenzofuran | dibenzofuran : A mancude organic heterotricyclic parent that consists of a furan ring flanked by two benzene rings ortho-fused across the 2,3- and 4,5-positions. dibenzofurans : Any organic heterotricyclic compound based on a dibenzofuran skeleton and its substituted derivatives thereof. Dibenzofurans: Compounds that include the structure of dibenzofuran. | dibenzofurans; mancude organic heterotricyclic parent; polycyclic heteroarene | xenobiotic |
| 3-methylcholanthrene | 3-methylcholanthrene : A pentacyclic ortho- and peri-fused polycyclic arene consisting of a dihydrocyclopenta[ij]tetraphene ring system with a methyl substituent at the 3-position. Methylcholanthrene: A carcinogen that is often used in experimental cancer studies. | ortho- and peri-fused polycyclic arene | aryl hydrocarbon receptor agonist; carcinogenic agent |
| 5,11-dihydroindolo[3,2-b]carbazole-12-carboxaldehyde | indolocarbazole | ||
| benzo(a)pyrene | Benzo(a)pyrene: A potent mutagen and carcinogen. It is a public health concern because of its possible effects on industrial workers, as an environmental pollutant, an as a component of tobacco smoke. benzo[a]pyrene : An ortho- and peri-fused polycyclic arene consisting of five fused benzene rings. | ortho- and peri-fused polycyclic arene | carcinogenic agent; mouse metabolite |
| beta-naphthoflavone | beta-naphthoflavone : An extended flavonoid resulting from the formal fusion of a benzene ring with the f side of flavone. beta-Naphthoflavone: A polyaromatic hydrocarbon inducer of P4501A1 and P4501A2 cytochromes. (Proc Soc Exp Biol Med 1994 Dec:207(3):302-308) | extended flavonoid; naphtho-gamma-pyrone; organic heterotricyclic compound | aryl hydrocarbon receptor agonist |
| bisacodyl | Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | diarylmethane | |
| kynurenic acid | kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4. Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool. | monohydroxyquinoline; quinolinemonocarboxylic acid | G-protein-coupled receptor agonist; human metabolite; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist; Saccharomyces cerevisiae metabolite |
| indigo | hydroxyindoles | ||
| 2,3,7,8-tetrachlorodibenzodioxine | Tetrachlorodibenzodioxin: A mixture of isomers. | polychlorinated dibenzodioxine | |
| 2,4,2',4'-tetrachlorobiphenyl | 2,2',4,4'-tetrachlorobiphenyl : A tetrachlorobiphenyl that is biphenyl in which each of the phenyl groups is substituted at positions 2 and 4 by chlorines. 2,4,2',4'-tetrachlorobiphenyl: structure | dichlorobenzene; tetrachlorobiphenyl | |
| octachlorodibenzo-4-dioxin | octachlorodibenzo-4-dioxin: RN given refers to unlabeled parent cpd | polychlorinated dibenzodioxine | |
| 2-chlorodibenzofuran | 2-chlorodibenzofuran: structure | ||
| 1,2,3,4-tetrachlorodibenzodioxin | 1,2,3,4-tetrachlorodibenzodioxin: structure given in first source | polychlorinated dibenzodioxine | |
| pcb 118 | dichlorobenzene; pentachlorobiphenyl; trichlorobenzene | ||
| 3,4,3',4'-tetrachlorobiphenyl | 3,3',4,4'-tetrachlorobiphenyl : A tetrachlorobiphenyl that is biphenyl in which the hydrogens at position 3 and 4 on each phenyl group are replaced by chlorines. 3,4,3',4'-tetrachlorobiphenyl: RN given refers to parent cpd | dichlorobenzene; tetrachlorobiphenyl | |
| 2,3,3',4,4'-pentachlorobiphenyl | dichlorobenzene; pentachlorobiphenyl; trichlorobenzene | ||
| 2,3,4,5-tetrachlorobiphenyl | tetrachlorobiphenyl : Any polychlorobiphenyl with molecular formula C12H6Cl4. | tetrachlorobenzene; tetrachlorobiphenyl | |
| 1,2,7,8-tetrachlorodibenzo-p-dioxin | 1,2,7,8-tetrachlorodibenzo-p-dioxin: structure in first source | ||
| 2,4,5,2',4',5'-hexachlorobiphenyl | hexachlorobiphenyl | ||
| 2,3,3',4,4',5-hexachlorobiphenyl | dichlorobenzene; hexachlorobiphenyl; tetrachlorobenzene | ||
| 2,8-dichlorodibenzo-4-dioxin | 2,8-dichlorodibenzo-4-dioxin: metabolite for 2,3,7,8-TCDD | ||
| 1,2,3,4,7,8-hexachlorodibenzodioxin | 1,2,3,4,7,8-hexachlorodibenzodioxin: structure given in first source | polychlorinated dibenzodioxine | |
| 1,2,4-trichlorodibenzo-1,4-dioxin | 1,2,4-trichlorodibenzo-1,4-dioxin: structure given in first source | ||
| 1,2,3,7,8-pentachlorodibenzo-p-dioxin | polychlorinated dibenzodioxine | ||
| 2,3,7,8-tetrabromodibenzo-4-dioxin | 2,3,7,8-tetrabromodibenzo-4-dioxin: structure given in first source 2,3,7,8-tetrabromodibenzodioxine : An organobromine compound that is dibenzodioxine carrying four bromo substituents at positions 2, 3, 7 and 8. | dibenzodioxine; organobromine compound | |
| 2,3,7,8-tetrachlorodibenzofuran | 2,3,7,8-tetrachlorodibenzofuran: toxic product which was generated in Italy due to an explosion in a plant manufacturing 2,4,5-trichlorophenol | polychlorinated dibenzofuran | |
| 2,3,4,7,8-pentachlorodibenzofuran | 2,3,4,7,8-pentachlorodibenzofuran: structure given in first source | polychlorinated dibenzofuran | |
| 1,2,3,7,8-pentachlorodibenzofuran | 1,2,3,7,8-pentachlorodibenzofuran: structure given in first source; RN given refers to parent cpd | polychlorinated dibenzofuran | |
| 1,2,3,4,7,8-hexachlorodibenzofuran | polychlorinated dibenzofuran | ||
| 2,3,4,4'5-pentachlorobiphenyl | monochlorobenzenes; pentachlorobiphenyl; tetrachlorobenzene | ||
| 3,4,5,3',4'-pentachlorobiphenyl | 3,3',4,4',5-pentachlorobiphenyl : A pentachlorobiphenyl in which the chlorines are located at the 3, 4, 5, 3', and 4' positions. | pentachlorobiphenyl; trichlorobenzene | |
| 6-methyl-1,3,8-trichlorodibenzofuran | 6-methyl-1,3,8-trichlorodibenzofuran: structure given in first source | ||
| kynurenine | L-kynurenine : A kynurenine that has L configuration. | amino acid zwitterion; kynurenine; non-proteinogenic L-alpha-amino acid | human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| 3-chlorodibenzofuran | 3-chlorodibenzofuran: structure given in first source | ||
| kaempferol | 7-hydroxyflavonol; flavonols; tetrahydroxyflavone | antibacterial agent; geroprotector; human blood serum metabolite; human urinary metabolite; human xenobiotic metabolite; plant metabolite | |
| 7-bromoindirubin-3'-oxime | 7-bromoindirubin-3'-oxime: has mild protein kinase inhibitory activity; induces caspase-independent cell death; structure in first source |