%0 Journal Article %T Inactivation of the Nuclear Orphan Receptor COUP-TFII by Small Chemicals %+ Institut de Génétique et Développement de Rennes (IGDR) %+ Récepteurs nucléaires, maladies cardiovasculaires et diabète - U 1011 (RNMCD) %+ Institut Européen de Génomique du Diabète - European Genomic Institute for Diabetes - FR 3508 (EGID) %+ Institute of Immunology %+ Slovak Academy of Science [Bratislava] (SAS) %A Le Guével, Rémy %A Oger, Frederik %A Martinez-Jimenez, Celia P. %A Bizot, Maud %A Gheeraert, Celine %A Firmin, François %A Ploton, Maheul %A Kretova, Miroslava %A Palierne, Gaëlle %A Staels, Bart %A Barath, Peter %A Talianidis, Iannis %A Lefebvre, Philippe %A Eeckhoute, Jérôme %A Salbert, Gilles %Z This work was funded by the European Community (QLG1-CT-2001-01513), the Centre National pour la Recherche Scientifique and the Ministère de l’Enseignement Supérieur et de la Recherche. This work was also supported by grants from “European Genomic Institute for Diabetes” (E.G.I.D., ANR-10-LABX-46). F.O. and C.G. were supported by OSEO-ANVAR (IT-DIAB). B.S. is a member of the Institut Universitaire de France. %< avec comité de lecture %@ 1554-8929 %J ACS Chemical Biology %I American Chemical Society %V 12 %N 3 %P 654-663 %8 2017-03-17 %D 2017 %R 10.1021/acschembio.6b00593 %M 28059499 %Z Life Sciences [q-bio]/Genetics %Z Chemical Sciences/Medicinal ChemistryJournal articles %X 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. %G English %2 https://univ-rennes.hal.science/hal-01497231/file/Le-Guevel%20et%20al.%20-%202017%20-%20Inactivation%20of%20the%20nuclear%20orphan%20receptor%20COUP-T.pdf %L hal-01497231 %U https://univ-rennes.hal.science/hal-01497231 %~ INSERM %~ RIIP %~ UNIV-RENNES1 %~ CNRS %~ RIIP_LILLE %~ IFR140 %~ IGDR %~ STATS-UR1 %~ IGDR-SPARTE %~ UR1-UFR-SVE %~ UR1-HAL %~ UR1-SDV %~ TEST-UNIV-RENNES %~ TEST-UR-CSS %~ UNIV-RENNES %~ UNIV-LILLE %~ TEST-HALCNRS %~ RNMCD %~ ANR %~ UR1-BIO-SA