Cyproterone acetate acts as a disruptor of the aryl hydrocarbon receptor

An aryl hydrocarbon receptor conformation acts as the functional core of nuclear dioxin signaling.

DNA-complexed heterodimers of the aryl hydrocarbon receptor (AhR) with the Ah receptor nuclear translocator (Arnt) are the molecular switches for nuclear signaling of 2,3,7, 8-tetrachlorodibenzo-p-dioxin (TCDD). AhR-Arnt heterodimers regulate genes involved in the metabolism of xenobiotics or fatty acids and various genes important for growth and differentiation. In this report several potent m...

Aryl Hydrocarbon Receptor Activation

Bis-aryloxadiazoles as effective activators of the aryl hydrocarbon receptor.

Bis-aryloxadiazoles are common scaffolds in medicinal chemistry due to their wide range of biological activities. Previously, we identified a 1,2,4-bis-aryloxadiazole that blocks mammary branching morphogenesis through activation of the aryl hydrocarbon receptor (AHR). In addition to defects in mammary differentiation, AHR stimulation induces toxicity in many other tissues. We performed a struc...

Antioxidant Functions of the Aryl Hydrocarbon Receptor

The aryl hydrocarbon receptor (AhR) is a transcription factor belonging to the basic helix-loop-helix/PER-ARNT-SIM family. It is activated by a variety of ligands, such as environmental contaminants like polycyclic aromatic hydrocarbons or dioxins, but also by naturally occurring compounds and endogenous ligands. Binding of the ligand leads to dimerization of the AhR with aryl hydrocarbon recep...

The Aryl Hydrocarbon Receptor and Tumor Immunity

The aryl hydrocarbon receptor (AhR) is an important cytosolic, ligand-dependent transcription factor. Emerging evidence suggests the promoting role of the AhR in the initiation, promotion, progression, invasion, and metastasis of cancer cells. Studies on various tumor types and tumor cell lines have shown high AhR expression, suggesting that AhR is activated constitutively in tumors and facilit...