The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that promotes the expression of phase I and II xenobiotic chemical metabolizing enzyme genes, including the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2. 5-fluoro 203 is a cytotoxic compound that at 1 μM activates AhR signaling, inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest. In certain ovarian, breast, kidney, and colorectal cancer cells, 5-fluoro 203 can increase the levels of reactive oxygen species as well as activate JNK, ERK, and p38 MAPK.
