Aryl Hydrocarbon Receptor Antagonists

Aryl hydrocarbon receptors (AHRs) are cytosolic transcription factors that exist bound to co-chaperones in the resting state (Hsp90, prostaglandin E synthase 3 and hepatitis B virus X-associated protein 2). Ligand binding causes the co-chaperones to dissociate, allowing AHR to translocate to the nucleus, dimerize with AHR nuclear translocator (ARNT) and alter transcription of target genes.

AHR is an evolutionary conserved receptor that has roles in cell proliferation and differentiation and induction of xenobiotic-metabolizing enzymes (for example CYP1A1). The human gene encoding the aryl hydrocarbon receptor has been localized to chromosome 7p15.