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Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors

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posted on 2013-01-10, 00:00 authored by Jun R. Huh, Erika E. Englund, Hang Wang, Ruili Huang, Pengxiang Huang, Fraydoon Rastinejad, James Inglese, Christopher P. Austin, Ronald L. Johnson, Wenwei Huang, Dan R. Littman
Retinoic acid-related orphan receptor RORγt plays a pivotal role in the differentiation of TH17 cells. Antagonizing RORγt transcriptional activity is a potential means to treat TH17-related autoimmune diseases. Herein, we describe the identification of a series of diphenylpropanamides as novel and selective RORγ antagonists. Diphenylpropanamide 4n inhibited the transcriptional activity of RORγt, but not RORα, in cells. In addition, it suppressed human TH17 cell differentiation at submicromolar concentrations.

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