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Open Access Green as soon as Postprint is submitted to ZB.
Inactivation of the Nuclear Orphan Receptor COUP-TFII by Small Chemicals.
ACS Chem. Biol. 12, 654-663 (2017)
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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Publication type
Article: Journal article
Document type
Scientific Article
ISSN (print) / ISBN
1554-8929
e-ISSN
1554-8937
Journal
ACS Chemical Biology
Quellenangaben
Volume: 12,
Issue: 3,
Pages: 654-663
Publisher
American Chemical Society (ACS)
Publishing Place
Washington
Non-patent literature
Publications
Reviewing status
Peer reviewed
Institute(s)
Helmholtz Pioneer Campus (HPC)