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CIA-1 is an inhibitor of the nuclear receptor COUP-TFII.

NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation[1].

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[1] Leiming Wang, et al. Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatment. Sci Adv. 2020 Apr 29;6(18):eaaz8031. DOI:10.1126/sciadv.aaz8031