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Inactivation of the Nuclear Orphan Receptor COUP-TFII by Small Chemicals

Abstract : Chicken ovalbumin upstream promoter-transcription factor II (COUP-TFII/NR2F2) is an orphan member of the nuclear receptor family of transcription factors whose activities are modulated upon binding of small molecules into an hydrophobic ligand-binding pocket (LBP). Although the LBP of COUP-TFII is filled with aromatic amino-acid side chains, alternative modes of ligand binding could potentially lead to regulation of the orphan receptor. Here, we screened a synthetic and natural compound library in a yeast one-hybrid assay and identified 4-methoxynaphthol as an inhibitor of COUP-TFII. This synthetic inhibitor was able to counteract processes either positively or negatively regulated by COUP-TFII in different mammalian cell systems. Hence, we demonstrate that the true orphan receptor COUP-TFII can be targeted by small chemicals which could be used to study the physiological functions of COUP-TFII or to counteract detrimental COUP-TFII activities in various pathological conditions.
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Submitted on : Thursday, June 1, 2017 - 11:23:18 AM
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Rémy Le Guével, Frederik Oger, Celia P. Martinez-Jimenez, Maud Bizot, Celine Gheeraert, et al.. Inactivation of the Nuclear Orphan Receptor COUP-TFII by Small Chemicals. ACS Chemical Biology, American Chemical Society, 2017, 12 (3), pp.654-663. ⟨10.1021/acschembio.6b00593⟩. ⟨hal-01497231⟩



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