Browse AHR

Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Basic function annotation.
> Subcellular Location, Domain and Function
> Gene Ontology
> KEGG and Reactome Pathway
> Subcellular Location, Domain and Function
 
Subcellular Location Cytoplasm. Nucleus. Note=Initially cytoplasmic; upon binding with ligand and interaction with a HSP90, it translocates to the nucleus.
Domain PF00010 Helix-loop-helix DNA-binding domain
PF00989 PAS fold
PF08447 PAS fold
Function

Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Involved in cell-cycle regulation. Likely to play an important role in the development and maturation of many tissues. Regulates the circadian clock by inhibiting the basal and circadian expression of the core circadian component PER1. Inhibits PER1 by repressing the CLOCK-ARNTL/BMAL1 heterodimer mediated transcriptional activation of PER1.

> Gene Ontology
 
Biological Process GO:0002694 regulation of leukocyte activation
GO:0006805 xenobiotic metabolic process
GO:0007623 circadian rhythm
GO:0009410 response to xenobiotic stimulus
GO:0009636 response to toxic substance
GO:0030522 intracellular receptor signaling pathway
GO:0030888 regulation of B cell proliferation
GO:0032922 circadian regulation of gene expression
GO:0032943 mononuclear cell proliferation
GO:0032944 regulation of mononuclear cell proliferation
GO:0042100 B cell proliferation
GO:0042113 B cell activation
GO:0046651 lymphocyte proliferation
GO:0048511 rhythmic process
GO:0050670 regulation of lymphocyte proliferation
GO:0050864 regulation of B cell activation
GO:0050865 regulation of cell activation
GO:0051249 regulation of lymphocyte activation
GO:0070661 leukocyte proliferation
GO:0070663 regulation of leukocyte proliferation
GO:0071466 cellular response to xenobiotic stimulus
Molecular Function GO:0004874 aryl hydrocarbon receptor activity
GO:0004879 RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding
GO:0008134 transcription factor binding
GO:0031072 heat shock protein binding
GO:0035326 enhancer binding
GO:0046982 protein heterodimerization activity
GO:0051879 Hsp90 protein binding
GO:0070888 E-box binding
GO:0098531 transcription factor activity, direct ligand regulated sequence-specific DNA binding
Cellular Component GO:0005667 transcription factor complex
GO:0034751 aryl hydrocarbon receptor complex
GO:0034752 cytosolic aryl hydrocarbon receptor complex
GO:0034753 nuclear aryl hydrocarbon receptor complex
GO:0043235 receptor complex
GO:0044445 cytosolic part
> KEGG and Reactome Pathway
 
KEGG -
Reactome R-HSA-8937144: Aryl hydrocarbon receptor signalling
R-HSA-211859: Biological oxidations
R-HSA-211897: Cytochrome P450 - arranged by substrate type
R-HSA-211976: Endogenous sterols
R-HSA-535734: Fatty acid, triacylglycerol, and ketone body metabolism
R-HSA-1430728: Metabolism
R-HSA-556833: Metabolism of lipids and lipoproteins
R-HSA-1989781: PPARA activates gene expression
R-HSA-211945: Phase 1 - Functionalization of compounds
R-HSA-400206: Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
R-HSA-211981: Xenobiotics
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Literatures that report relations between AHR and anti-tumor immunity. The specific mechanism were also collected if the literature reports that a gene specifically promotes or inhibits the infiltration or function of T/NK cells.
> Text Mining
 
  Literatures describing the relation between AHR and anti-tumor immunity in human cancer.
PMID Cancer type Relation to immunity Evidence sentences
23144293Brain neoplasmInhibit immunityFurther, it was also recently shown that TDO-2-dependent production of KYN by brain tumors might be a novel mechanism for suppressing antitumor immunity and supporting tumor growth through the activation of the Aryl hydrocarbon receptor (AhR). This newly identified TDO-2-KYN-AhR signaling pathway opens up exciting future research opportunities and may represent a novel therapeutic target in cancer therapy.
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content High-throughput screening data (e.g. CRISPR-Cas9, shRNA and RNAi) for T cell-mediated killing. Genetic screen techniques can identify mechanisms of tumor cell resistance (e.g., PTPN2) and sensitivity (e.g., APLNR) to killing by cytotoxic T cells, the central effectors of anti-tumor immunity. After comprehensively searching, eight groups of screening data sets were collected in the current database. In this tab, users can check whether their selected genes cause resistance or increase sensitivity to T cell-mediated killing in various data sets.
> High-throughput Screening
  Statistical results of AHR in screening data sets for detecting immune reponses.
PMID Screening System Cancer Type Cell Line Data Set Statistical Results Relation to immunity
29301958CRISPR-Cas9 melanomaB16F10Pmel-1 T cell NA/NSNA/NS
29301958CRISPR-Cas9 melanomaB16F10OT-1 T cell NA/NSNA/NS
28783722CRISPR-Cas9 melanomaMel6242CT-CRISPR NA/NSNA/NS
28723893CRISPR-Cas9 melanomaB16GVAX+Anti-PD1 NA/NSNA/NS
28723893CRISPR-Cas9 melanomaB16GVAX NA/NSNA/NS
25691366RNAiBreast cancerMCF7Luc-CTL assay NA/NSNA/NS
24476824shRNAmelanomaB16Primary screen NA/NSNA/NS
24476824shRNAmelanomaB16Secondary screen NA/NSNA/NS
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Transcriptomic and genomic profiling of pre-treated tumor biopsies from responders and non-responders to immunotherapy. These data were used to identify signatures and mechanisms of response to checkpoint blockade (e.g., anti-PDL1 and anti-PD1). One example is that mutations in the gene PBRM1 benefit clinical survival of patients with clear cell renal cell carcinoma. After comprehensively searching, we collected 5 and 6 of transcriptomic and genomic data sets, respectively. In this tab, users can check whether their selected genes have significant difference of expression or mutation between responders and non-responders in various data sets.
> Expression difference between responders and non-responders
> Mutation difference between responders and non-responders
> Expression difference between responders and non-responders
 
Points in the above scatter plot represent the expression difference of AHR in various data sets.
No PMID Cancer type Group Drug # Res # NRes Log2 (Fold Change) P value Anno
126997480MelanomaallAnti-PD-1 (pembrolizumab and nivolumab)14120.0160.974
226997480MelanomaMAPKiAnti-PD-1 (pembrolizumab and nivolumab)65-0.4760.822
326997480Melanomanon-MAPKiAnti-PD-1 (pembrolizumab and nivolumab)870.3870.783
428552987Urothelial cancerallAnti-PD-L1 (atezolizumab) 9160.0950.856
528552987Urothelial cancersmokingAnti-PD-L1 (atezolizumab) 59-0.7370.775
628552987Urothelial cancernon-smokingAnti-PD-L1 (atezolizumab) 471.1380.713
729033130MelanomaallAnti-PD-1 (nivolumab) 26230.2460.634
829033130MelanomaNIV3-PROGAnti-PD-1 (nivolumab) 1511-0.0610.976
929033130MelanomaNIV3-NAIVEAnti-PD-1 (nivolumab) 11120.6330.771
1029301960Clear cell renal cell carcinoma (ccRCC)allAnti-PD-1 (nivolumab) 480.650.509
1129301960Clear cell renal cell carcinoma (ccRCC)VEGFRiAnti-PD-1 (nivolumab) 2001
1229301960Clear cell renal cell carcinoma (ccRCC)non-VEGFRiAnti-PD-1 (nivolumab) 281.0940.503
1329443960Urothelial cancerallAnti-PD-L1 (atezolizumab) 68230-0.1250.293
> Mutation difference between responders and non-responders
 
Points in the above scatter plot represent the mutation difference of AHR in various data sets.
No PMID Cancer type Group Drug # Res # NRes % Mut/Res % Mut/NRes % Diff (R vs NR) Pval Anno
125765070Non-small cell lung cancer (NSCLC)allAnti-PD-1 (pembrolizumab) 14170001
225765070Non-small cell lung cancer (NSCLC)smokingAnti-PD-1 (pembrolizumab) 1030001
325765070Non-small cell lung cancer (NSCLC)non-smokingAnti-PD-1 (pembrolizumab) 4140001
426359337MelanomaallAnti-CTLA-4 (ipilimumab) 27733.72.711
526359337MelanomaBRAFiAnti-CTLA-4 (ipilimumab) 0140001
626359337Melanomanon-BRAFiAnti-CTLA-4 (ipilimumab) 27593.73.40.31
726997480MelanomaallAnti-PD-1 (pembrolizumab and nivolumab)2117190190.113
826997480MelanomaMAPKiAnti-PD-1 (pembrolizumab and nivolumab)86250250.473
926997480Melanomanon-MAPKiAnti-PD-1 (pembrolizumab and nivolumab)131115.4015.40.482
1028552987Urothelial cancerallAnti-PD-L1 (atezolizumab) 9160001
1128552987Urothelial cancersmokingAnti-PD-L1 (atezolizumab) 590001
1228552987Urothelial cancernon-smokingAnti-PD-L1 (atezolizumab) 470001
1329033130MelanomaallAnti-PD-1 (nivolumab) 38272.602.61
1429033130MelanomaNIV3-PROGAnti-PD-1 (nivolumab) 22134.504.51
1529033130MelanomaNIV3-NAIVEAnti-PD-1 (nivolumab) 16140001
1629301960Clear cell renal cell carcinoma (ccRCC)allAnti-PD-1 (nivolumab) 11139.109.10.458
1729301960Clear cell renal cell carcinoma (ccRCC)VEGFRiAnti-PD-1 (nivolumab) 610001
1829301960Clear cell renal cell carcinoma (ccRCC)non-VEGFRiAnti-PD-1 (nivolumab) 512200200.294
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between abundance of tumor-infiltrating lymphocytes (TILs) and expression, copy number, methylation, or mutation of AHR. The immune-related signatures of 28 TIL types from Charoentong's study, which can be viewed in the download page. For each cancer type, the relative abundance of TILs were inferred by using gene set variation analysis (GSVA) based on gene expression profile. In this tab, users can examine which kinds of TILs might be regulated by the current gene.
> Lymphocyte
 
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between three kinds of immunomodulators and expression, copy number, methylation, or mutation of AHR. These immunomo-dulators were collected from Charoentong's study. In this tab, users can examine which immunomodulators might be regulated by AHR.
> Immunoinhibitor
> Immunostimulator
> MHC molecule
> Immunoinhibitor
 
> Immunostimulator
 
> MHC molecule
 
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between chemokines (or receptors) and expression, copy number, methylation, or mutation of AHR. In this tab, users can examine which chemokines (or receptors) might be regulated by the current gene.
> Chemokine
> Receptor
> Chemokine
 
> Receptor
 
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Distribution of AHR expression across immune and molecular subtypes.
> Immune subtype
> Molecular subtype
> Immune subtype
 
> Molecular subtype
 
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Associations between AHR and clinical features.
> Overall survival analysis
> Cancer stage
> Tumor grade
> Overall survival
 
> Stage
 
> Grade
 
Summary
SymbolAHR
Namearyl hydrocarbon receptor
Aliases bHLHe76; AH-receptor; ah receptor; aromatic hydrocarbon receptor; class E basic helix-loop-helix protein 76
Chromosomal Location7p15
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Drugs targeting AHR collected from DrugBank database.
> Drugs from DrugBank database
 

  Details on drugs targeting AHR.
ID Name Drug Type Targets #Targets
DB00338OmeprazoleSmall MoleculeAHR, ATP4A2
DB00379MexiletineSmall MoleculeAHR, SCN5A2
DB00393NimodipineSmall MoleculeAHR, CACNA1C, CACNA1D, CACNA1F, CACNA1S, CACNB1, CACNB2, CACNB3, C ......10
DB00499FlutamideSmall MoleculeAHR, AR, NR1I23
DB01076AtorvastatinSmall MoleculeAHR, DPP4, HMGCR3
DB01097LeflunomideSmall MoleculeAHR, DHODH, PTK2B3
DB01404GinsengSmall MoleculeAHR, IL6, PTGS23
DB02052Indirubin-3'-MonoximeSmall MoleculeAHR, CDK1, CDK2, CDK5, CDK5R1, GSK3B6
DB02709ResveratrolSmall MoleculeAHR, AKT1, ALOX15, ALOX5, APP, CBR1, CLEC14A, CSNK2A1, ESR1, ITGA5 ......25
DB04216QuercetinSmall MoleculeACTB, AHR, ATP5A1, ATP5B, ATP5C1, CBR1, CEBPB, CSNK2A1, CSNK2B, CY ......27
DB06732beta-NaphthoflavoneSmall MoleculeAHR, CYP1B1, ESR1, ESRRA, NR2F15
DB07715EmodinSmall MoleculeAHR, CSNK2A12
DB08624BENZOTHIAZOLESmall MoleculeAHR, F22
DB08995DiosminSmall MoleculeAHR1
DB11577Indigotindisulfonic AcidSmall MoleculeAHR1
DB11937Kynurenic AcidSmall MoleculeAHR, GPR352
DB12116Epigallocatechin GallateSmall MoleculeAHR, DHFRL1, DNMT13
DB12328CantharidinSmall MoleculeAHR1
DB12379IndirubinSmall MoleculeAHR, CYP1A12