Inactivation of the Nuclear Orphan Receptor COUP-TFII by Small Chemicals - Université de Rennes Accéder directement au contenu
Article Dans Une Revue ACS Chemical Biology Année : 2017

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

Résumé

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.
Le-Guevel et al. - 2017 - Inactivation of the nuclear orphan receptor COUP-T.pdf (11.99 Mo) Télécharger le fichier
supp-data-cb6b00593_si_001.pdf (3.25 Mo) Télécharger le fichier
Origine : Fichiers produits par l'(les) auteur(s)
Origine : Fichiers produits par l'(les) auteur(s)

Dates et versions

hal-01497231 , version 1 (01-06-2017)

Identifiants

Citer

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, 2017, 12 (3), pp.654-663. ⟨10.1021/acschembio.6b00593⟩. ⟨hal-01497231⟩
167 Consultations
400 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More