Benzoxazepines Achieve Potent Suppression of IL-17 Release in Human T-Helper 17 (TH17) Cells through an Induced-Fit Binding Mode to the Nuclear Receptor RORγ

RORγt, an isoform of the retinoic acid‐related orphan receptor gamma (RORc, RORγ), has been identified as the master regulator of T‐helper 17 (TH17) cell function and development, making it an attractive target for the treatment of autoimmune diseases. Validation for this target comes from antibodie...

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Veröffentlicht in:	ChemMedChem 2016-01, Vol.11 (2), p.207-216
Hauptverfasser:	Olsson, Roine I., Xue, Yafeng, von Berg, Stefan, Aagaard, Anna, McPheat, Jane, Hansson, Eva L., Bernström, Jenny, Hansson, Pia, Jirholt, Johan, Grindebacke, Hanna, Leffler, Agnes, Chen, Rongfeng, Xiong, Yao, Ge, Hongbin, Hansson, Thomas G., Narjes, Frank
Format:	Artikel
Sprache:	eng
Schlagworte:	autoimmune diseases Binding Sites - drug effects cocrystal structures Dose-Response Relationship, Drug Humans interleukin 17 (IL-17) Interleukin-17 - immunology Interleukin-17 - secretion inverse agonists Models, Molecular Molecular Structure Nuclear Receptor Subfamily 1, Group F, Member 3 - metabolism nuclear receptors Oxazepines - chemical synthesis Oxazepines - chemistry Oxazepines - pharmacology Protein Binding - drug effects RORγ Structure-Activity Relationship TH17 cells Th17 Cells - drug effects Th17 Cells - immunology Th17 Cells - metabolism
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