Aryl hydrocarbon receptor

Target id: 2951

Nomenclature: Aryl hydrocarbon receptor

Family: Aryl hydrocarbon receptor complex

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Aryl hydrocarbon receptor has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 838 7p21.1 AHR aryl hydrocarbon receptor
Mouse - 839 12 A3 Ahr aryl-hydrocarbon receptor
Rat - 844 6q16 Ahr aryl hydrocarbon receptor
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the AHR-ARNT heterodimer in complex with the DRE
PDB Id:  5V0L
Resolution:  4.0Å
Species:  Human
References:  3

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
tapinarof Hs Agonist 6.7 – 7.0 pKd 4
pKd 6.7 – 7.0 (Kd 2x10-7 – 1x10-7 M) [4]
Description: Direct binding of tapinarof to the AhR-ARNT heterodimer by fluorescence assay.
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
TCDD Hs Binding - -
Immunopharmacology Comments
The AhR is a critical regulator of innate and adaptive immune responses that influences the balance of Th17 and Treg cells [2]. It is widely expressed in the skin where it is important for the development and maintenance of the skin barrier. AhR agonists are now being exploited for immunomodulatory potential, particulary for anti-inflammatory activity [1] in skin diseases like psoriasis and atopic dermatitis (see tapinarof for example [4]).
Immuno Process Associations
Immuno Process:  B cell (activation)
Immuno Process ID:  5
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  regulation of B cell proliferation (GO:0030888) IDA
References: 
Immuno Process:  Immune regulation
Immuno Process ID:  6
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  regulation of B cell proliferation (GO:0030888) IDA
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  regulation of B cell proliferation (GO:0030888) IDA
References: 
General Comments
The AhR is a cytosolic ligand-activated transcription factor. It senses a wide range of endogenous and exogenous molecules, recruiting downstream pathways that impact on a variety of biological processes.

References

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1. Di Meglio P, Duarte JH, Ahlfors H, Owens ND, Li Y, Villanova F, Tosi I, Hirota K, Nestle FO, Mrowietz U et al.. (2014) Activation of the aryl hydrocarbon receptor dampens the severity of inflammatory skin conditions. Immunity40 (6): 989-1001. [PMID:24909886]

2. Mascanfroni ID, Takenaka MC, Yeste A, Patel B, Wu Y, Kenison JE, Siddiqui S, Basso AS, Otterbein LE, Pardoll DM et al.. (2015) Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α. Nat. Med.21 (6): 638-46. [PMID:26005855]

3. Seok SH, Lee W, Jiang L, Molugu K, Zheng A, Li Y, Park S, Bradfield CA, Xing Y. (2017) Structural hierarchy controlling dimerization and target DNA recognition in the AHR transcriptional complex. Proc. Natl. Acad. Sci. U.S.A.114 (21): 5431-5436. [PMID:28396409]

4. Smith SH, Jayawickreme C, Rickard DJ, Nicodeme E, Bui T, Simmons C, Coquery CM, Neil J, Pryor WM, Mayhew D et al.. (2017) Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J. Invest. Dermatol.137 (10): 2110-2119. [PMID:28595996]

How to cite this page

Aryl hydrocarbon receptor complex: Aryl hydrocarbon receptor. Last modified on 24/10/2017. Accessed on 16/01/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2951.