Molecular mechanisms of AhR functions in the regulation of cytochrome P450 genes

Transcriptional Factor Aryl Hydrocarbon Receptor (Ahr) Controls Cardiovascular and Respiratory Functions by Regulating the Expression of the Vav3 Proto-oncogene

“…S1D). These results indicate that, unlike other Ahr transcriptional targets (1,4), the regulation of the constitutive expression of the Vav3 proto-oncogene does not seem to entail activation of Ahr by xenobiotics.…”

“…This molecule has attracted a lot of attention in the toxicology field because it acts as the main intracellular target for polycyclic and halogenated aromatic environmental pollutants such as benzo[a]pyrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin (1,3,4). Activation of Ahr by those drugs induces the transcription of genes containing XRE sites in their promoter regions (1,4).…”

“…This molecule has attracted a lot of attention in the toxicology field because it acts as the main intracellular target for polycyclic and halogenated aromatic environmental pollutants such as benzo[a]pyrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin (1,3,4). Activation of Ahr by those drugs induces the transcription of genes containing XRE sites in their promoter regions (1,4). Known Ahr targets include loci encoding cytochrome P450 family members in charge of the phase I detoxification response (5-9), phase II detoxification proteins (10 -12), metabolism-related enzymes (13)(14)(15), and many other molecules (16,17).…”

The Kidney and Uremic Toxin Removal: Glomerulus or Tubule?

“…XRE generally is recognized by the Aryl hydrocarbon receptor (AhR) and the AhR nuclear translocator heterodimer. 57 AhR binds classic ligands of environmental pollutants such as halogenated aromatic hydrocarbons (eg, benzopyrene, 3-methylcholanthrene, and the foxglove plant-derivative [and cardioselective drug] digoxin). 58 Human SLCO4C1 promoter activity was increased by 3-methylcholanthrene.…”

Phosphodiesterases link the aryl hydrocarbon receptor complex to cyclic nucleotide signaling

“…The classical pathway for AHR activation is initiated by binding of membrane-permeable ligands, such as TCDD, to AHR. Ligand binding to AHR probably exposes the nuclear localization sequence and the ligand-activated AHR complex translocates into the nucleus and forms a heterodimer with the closely related protein ARNT (AHR nuclear translocator, also known as HIF-1β), with the concurrent loss of HSP90, XAP2, and p23 from the complex [11,12]. The AHR/ARNT heterodimer forms the functional transcription factor complex that recruits other co-activator molecules and chromatin remodelling enzymes [10,13].…”