1057 Vemurafenib acts as an aryl hydrocarbon receptor antagonist

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...

Aryl Hydrocarbon Receptor and Stem Cells

From the biochemical point of view, the aryl hydrocarbon receptor (AHR) is a highly conserved, developmentally regulated, and ligand-activated member of the bHLH/PAS family of transcription factors. The AHR was originally discovered because of the human and animal toxicity of its most potent and persistent ligand, 2,3,7,8-tetrachlorodibenzo-pdioxin, usually just referred to as “dioxin.” The can...

Aryl hydrocarbon receptor and lung cancer.

The leading cause of lung cancer is exposure to cigarette smoke and other environmental pollutants, which include formaldehyde, acrolein, benzene, dioxin, and polycyclic aromatic hydrocarbons (PAHs). PAHs and dioxins are exogenous ligands that directly bind to the aryl hydrocarbon receptor (AhR), a transcription factor that activates xenobiotic metabolism, histone modification (an important ste...