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The inhibitor specifically suppressed COUP-TFII activity to modify its target genetics. Mechanistically, the inhibitor right bound to the COUP-TFII ligand-binding domain and disrupted COUP-TFII relationship with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene legislation. Through blocking COUP-TFII's oncogenic activity in prostate cancer tumors, the inhibitor efficiently exerted a potent antitumor effect in xenograft mouse models and patient-derived xenograft models. Our stu