HIGHLIGHTS
SUMMARY
Carvones do not displace radiolabeled ligands from binding to AhR but instead bind allosterically within the bHLH/PAS-A region of AhR. Carvones do not influence the translocation of ligand-activated AhR into the nucleus but inhibit the heterodimerization of AhR with its canonical partner ARNT and subsequent binding of AhR to the promoter of CYP1A1. The antagonist effects of carvones and CH223191 (orthosteric AhR antagonist) on agonist-inducible AhR activity were examined in cells co-incubated for 4 h and 24 h with a fixed concentration of agonist ligands (corresponding to their EC80 . . .
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