Target intelligence / Profile preview

Aryl hydrocarbon receptor (AhR)

Target
AhR
Molecular classification
Transcription factor, bHLH/PAS superfamily, Receptor
01

Overview

The Aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor belonging to the bHLH/PAS superfamily. It plays a crucial role in sensing environmental chemicals (xenobiotics) and endogenous metabolites, regulating gene expression in response. Upon ligand binding, AhR translocates to the nucleus, dimerizes with ARNT, and binds to XRE/DRE sequences, modulating the transcription of target genes involved in xenobiotic metabolism, immune function, development, and other processes. Dysregulation of AhR is implicated in various diseases, including immunotoxicity, cancer, and developmental abnormalities.

Other names
AHRahrahRdioxin receptor
02

Mechanism of action

Ligand binding to AhR induces a conformational change, leading to dissociation from chaperone proteins (Hsp90, XAP2/AIP/ARA9, p23), translocation to the nucleus, dimerization with ARNT, binding to XRE/DRE sequences on DNA, and regulation of target gene transcription (e.g., CYP1A1, CYP1B1).

03

Biological functions

Xenobiotic metabolismImmune regulationVascular developmentCardiac developmentCellular differentiationStem cell maintenanceGene transcription regulation
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Disease associations

ImmunotoxicityCancer susceptibilityDevelopmental defectsAltered xenobiotic metabolism disordersImmune dysfunctions
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Safety considerations

Immunotoxicity due to aberrant activationIncreased susceptibility to certain cancersDevelopmental abnormalitiesDysregulation can lead to various disorders
06

Interacting drugs

Polycyclic aromatic hydrocarbons

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