N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists

The nuclear retinoic acid receptor‐related orphan receptor γ (RORγ; NR1F3) is a key regulator of inflammatory gene programs involved in T helper 17 (TH17) cell proliferation. As such, synthetic small‐molecule repressors (inverse agonists) targeting RORγ have been extensively studied for their potent...

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Veröffentlicht in:	ChemMedChem 2016-12, Vol.11 (23), p.2607-2620
Hauptverfasser:	Doebelin, Christelle, Patouret, Rémi, Garcia-Ordonez, Ruben D., Chang, Mi Ra, Dharmarajan, Venkatasubramanian, Kuruvilla, Dana S., Novick, Scott J., Lin, Li, Cameron, Michael D., Griffin, Patrick R., Kamenecka, Theodore M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Autoimmune diseases Binding Sites Cancer immunotherapy Cell activation Cell growth Cell proliferation Chemical compounds Coordination compounds Deuterium Drug Inverse Agonism HEK293 Cells Helper cells Heterocyclic compounds Humans Hydrogen-deuterium exchange Immune response Immune system Immunotherapy Indoles - chemical synthesis Indoles - chemistry Indoles - metabolism Inflammation Interleukin-17 - genetics Interleukin-17 - metabolism Inverse agonists Lymphocytes T Mass spectrometry Mass spectroscopy Molecular Docking Simulation N-arylsulfonyl indolines nuclear receptors Pharmacology Promoter Regions, Genetic Protein Binding Protein Structure, Tertiary Receptors Receptors, Retinoic Acid - agonists Receptors, Retinoic Acid - metabolism Repressors Retinoic acid Retinoic Acid Receptor gamma RORγ agonists Structure-Activity Relationship Th17 Cells - cytology Th17 Cells - immunology Th17 Cells - metabolism
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