Page last updated: 2024-08-07 13:15:27
Aryl hydrocarbon receptor
An aryl hydrocarbon receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P35869]
Synonyms
Ah receptor;
AhR;
Class E basic helix-loop-helix protein 76;
bHLHe76
Research
Bioassay Publications (12)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (8.33) | 18.2507 |
| 2000's | 3 (25.00) | 29.6817 |
| 2010's | 4 (33.33) | 24.3611 |
| 2020's | 4 (33.33) | 2.80 |
Compounds (36)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dibenzofuran | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 3-methylcholanthrene | Homo sapiens (human) | EC50 | 0.4900 | 1 | 1 |
| 5,11-dihydroindolo[3,2-b]carbazole-12-carboxaldehyde | Homo sapiens (human) | EC50 | 4.5310 | 2 | 2 |
| benzo(a)pyrene | Homo sapiens (human) | EC50 | 1.3525 | 2 | 2 |
| beta-naphthoflavone | Homo sapiens (human) | EC50 | 1.0521 | 4 | 4 |
| bisacodyl | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| kynurenic acid | Homo sapiens (human) | EC50 | 0.3000 | 1 | 1 |
| indigo | Homo sapiens (human) | EC50 | 1.7000 | 1 | 1 |
| 2,3,7,8-tetrachlorodibenzodioxine | Homo sapiens (human) | EC50 | 0.0100 | 1 | 1 |
| 2,4,2',4'-tetrachlorobiphenyl | Homo sapiens (human) | EC50 | 130.0170 | 1 | 1 |
| octachlorodibenzo-4-dioxin | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| 2-chlorodibenzofuran | Homo sapiens (human) | EC50 | 279.8980 | 1 | 1 |
| 1,2,3,4-tetrachlorodibenzodioxin | Homo sapiens (human) | EC50 | 1.3002 | 1 | 1 |
| pcb 118 | Homo sapiens (human) | EC50 | 9.0991 | 1 | 1 |
| 3,4,3',4'-tetrachlorobiphenyl | Homo sapiens (human) | EC50 | 0.7096 | 1 | 1 |
| 2,3,3',4,4'-pentachlorobiphenyl | Homo sapiens (human) | EC50 | 4.2658 | 1 | 1 |
| 2,3,4,5-tetrachlorobiphenyl | Homo sapiens (human) | EC50 | 139.9590 | 1 | 1 |
| 1,2,7,8-tetrachlorodibenzo-p-dioxin | Homo sapiens (human) | EC50 | 0.1600 | 1 | 1 |
| 2,4,5,2',4',5'-hexachlorobiphenyl | Homo sapiens (human) | EC50 | 79.4328 | 1 | 1 |
| 2,3,3',4,4',5-hexachlorobiphenyl | Homo sapiens (human) | EC50 | 7.0958 | 1 | 1 |
| 2,8-dichlorodibenzo-4-dioxin | Homo sapiens (human) | EC50 | 3.1989 | 1 | 1 |
| 1,2,3,4,7,8-hexachlorodibenzodioxin | Homo sapiens (human) | EC50 | 0.2799 | 1 | 1 |
| 1,2,4-trichlorodibenzo-1,4-dioxin | Homo sapiens (human) | EC50 | 13.0017 | 1 | 1 |
| 1,2,3,7,8-pentachlorodibenzo-p-dioxin | Homo sapiens (human) | EC50 | 0.0794 | 1 | 1 |
| 2,3,7,8-tetrabromodibenzo-4-dioxin | Homo sapiens (human) | EC50 | 0.0015 | 1 | 1 |
| 2,3,7,8-tetrachlorodibenzofuran | Homo sapiens (human) | EC50 | 0.0410 | 1 | 1 |
| 2,3,4,7,8-pentachlorodibenzofuran | Homo sapiens (human) | EC50 | 0.0151 | 1 | 1 |
| 1,2,3,7,8-pentachlorodibenzofuran | Homo sapiens (human) | EC50 | 0.0741 | 1 | 1 |
| 1,2,3,4,7,8-hexachlorodibenzofuran | Homo sapiens (human) | EC50 | 0.2301 | 1 | 1 |
| 2,3,4,4'5-pentachlorobiphenyl | Homo sapiens (human) | EC50 | 4.1020 | 1 | 1 |
| 3,4,5,3',4'-pentachlorobiphenyl | Homo sapiens (human) | EC50 | 0.1300 | 1 | 1 |
| 6-methyl-1,3,8-trichlorodibenzofuran | Homo sapiens (human) | EC50 | 0.0490 | 1 | 1 |
| 6-methyl-1,3,8-trichlorodibenzofuran | Homo sapiens (human) | Kd | 0.0001 | 1 | 1 |
| 3-chlorodibenzofuran | Homo sapiens (human) | EC50 | 41.9759 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| beta-naphthoflavone | Homo sapiens (human) | Concentration | 100.0000 | 1 | 1 |
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.Bioorganic & medicinal chemistry, , Volume: 18, Issue:3, 2010
An electrochemical device for the assay of the interaction between a dioxin receptor and its various ligands.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Enables
This protein enables 16 target(s):
| Target | Category | Definition |
|---|
| transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
| DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
| cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site, located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by some RNA polymerase. Cis-regulatory sites are often referred to as a sequence motifs, enhancers, or silencers. [GOC:txnOH-2018] |
| TFIID-class transcription factor complex binding | molecular function | Binding to a general RNA polymerase II transcription factor belonging to the TFIID complex, one of the factors involved in formation of the preinitiation complex (PIC) by RNA polymerase II. [GOC:krc, PMID:16858867] |
| transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
| nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| TBP-class protein binding | molecular function | Binding to a member of the class of TATA-binding proteins (TBP), including any of the TBP-related factors (TRFs). [GOC:jl, GOC:txnOH, http://www.mblab.gla.ac.uk/, PMID:16858867] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| Hsp90 protein binding | molecular function | Binding to Hsp90 proteins, any of a group of heat shock proteins around 90kDa in size. [GOC:ai] |
| RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
| E-box binding | molecular function | Binding to an E-box, a DNA motif with the consensus sequence CANNTG that is found in the promoters of a wide array of genes expressed in neurons, muscle and other tissues. [GOC:BHF, GOC:vk, PMID:11812799] |
| sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 6 target(s):
| Target | Category | Definition |
|---|
| nuclear aryl hydrocarbon receptor complex | cellular component | An aryl hydrocarbon receptor (AhR) complex found in the nucleus; ; consists of ligand-bound AhR and the aryl hydrocarbon receptor nuclear translocator (ARNT). [PMID:7598497] |
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
| transcription regulator complex | cellular component | A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl] |
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
| cytosolic aryl hydrocarbon receptor complex | cellular component | 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] |
| aryl hydrocarbon receptor complex | cellular component | A protein complex that acts as an aryl hydrocarbon (Ah) receptor. Cytosolic and nuclear Ah receptor complexes have different subunit composition, but both contain the ligand-binding subunit AhR. [GOC:mah, PMID:7598497] |
Involved In
This protein is involved in 22 target(s):
| Target | Category | Definition |
|---|
| blood vessel development | biological process | The process whose specific outcome is the progression of a blood vessel over time, from its formation to the mature structure. The blood vessel is the vasculature carrying blood. [GOC:hjd, UBERON:0001981] |
| regulation of adaptive immune response | biological process | Any process that modulates the frequency, rate, or extent of an adaptive immune response. [GOC:add] |
| negative regulation of T cell mediated immune response to tumor cell | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of a T cell mediated immune response to tumor cell. [GOC:add] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| response to toxic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a toxic stimulus. [GOC:lr] |
| regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| cAMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic AMP (cAMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |
| intracellular receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a receptor located within a cell. [GOC:bf, GOC:mah] |
| regulation of B cell proliferation | biological process | Any process that modulates the frequency, rate or extent of B cell proliferation. [GOC:mah] |
| circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
| negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| negative regulation of inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| cellular response to molecule of bacterial origin | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus by molecules of bacterial origin such as peptides derived from bacterial flagellin. [GOC:mah] |
| cellular response to cAMP | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:mah] |
| cellular response to forskolin | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a forskolin stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:15937517] |
| cellular response to 2,3,7,8-tetrachlorodibenzodioxine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a 2,3,7,8-tetrachlorodibenzodioxine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23196670] |