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Copyright ©The Author(s) 2024.
World J Exp Med. Sep 20, 2024; 14(3): 96269
Published online Sep 20, 2024. doi: 10.5493/wjem.v14.i3.96269
Table 2 Mechanisms of action and potential effects of promising aryl hydrocarbon receptor antagonists on malignancies
AhR ligands
Mechanism of action
Potential effects on malignancies
Ref.
Natural products
CurcuminCompetitive binding to the AhR ligand-binding domainSuppresses proliferation, migration, and invasion of cancer cells; may enhance anti-tumor immunity[54,62,63]
QuercetinCompetitive binding to the AhR ligand-binding domain; may also inhibit AhR nuclear translocationSuppresses proliferation and induces apoptosis in cancer cells[55]
ResveratrolMay interfere with AhR-DNA binding; may also possess antioxidant and anti-inflammatory propertiesMay inhibit tumor growth and metastasis[55,64]
Synthetic ligands
CH-223191Competitive binding to the AhR ligand-binding domainSuppresses proliferation and migration of cancer cells[65]
NH3 (Ammonia)Competitive binding to the AhR ligand-binding domainShows promise in preclinical models, but may have limitations due to potential toxicity[66]
Small molecule antagonistsCompetitive binding to the AhR ligand-binding domain or interfering with AhR dimerizationSeveral novel small molecules are under development, with preclinical studies ongoing[67,68]