Development of novel aryl hydrocarbon receptor antagonists

Development of novel CH223191-based antagonists of the aryl hydrocarbon receptor.

Aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that regulates genes involved in drug/xenobiotic metabolism, cell cycle progression, cell fate determination, immune function, and inflammatory response. Increasing evidence that AHR plays a role in the pathophysiology of a number of human disease states is driving the need for improved pharmacological tools to be used f...

Aryl Hydrocarbon Receptor Activation

tert-Butylhydroquinone is a novel aryl hydrocarbon receptor ligand.

In contrast to the beneficial effects of tert-butylhydroquinone (tBHQ) as a food antioxidant, a number of studies have shown that chronic exposure to tBHQ may induce carcinogenicity. Therefore, we examined the ability of tBHQ to induce the cytochrome P450 1a1 (Cyp1a1), an enzyme known to play an important role in the chemical activation of xenobiotics to carcinogenic derivatives. A significant ...

Ginsenosides Are Novel Naturally-Occurring Aryl Hydrocarbon Receptor Ligands

The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor that mediates many of the biological and toxicological actions of structurally diverse chemicals. In this study, we examined the ability of a series of ginsenosides extracted from ginseng, a traditional Chinese medicine, to bind to and activate/inhibit the AHR and AHR signal transduction. Utilizing a combination of l...

Development of novel oestrogen-receptor antagonists.

as osteoporosis. Nevertheless, in time, tamoxifenresistant tumours often arise in patients and some of these could benefit from treatment with an antioestrogen, the mechanism of action of which is different from that of tamoxifen. It is important to establish whether other anti-oestrogens function by one or other of the mechanisms suggested for tamoxifen and ICI 164384 or by another novel means...