Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors 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 10.1021/ml300286h.s001 https://acs.figshare.com/articles/journal_contribution/Identification_of_Potent_and_Selective_Diphenylpropanamide_ROR_Inhibitors/2453470 Retinoic acid-related orphan receptor RORγt plays a pivotal role in the differentiation of T<sub>H</sub>17 cells. Antagonizing RORγt transcriptional activity is a potential means to treat T<sub>H</sub>17-related autoimmune diseases. Herein, we describe the identification of a series of diphenylpropanamides as novel and selective RORγ antagonists. Diphenylpropanamide <b>4n</b> inhibited the transcriptional activity of RORγt, but not RORα, in cells. In addition, it suppressed human T<sub>H</sub>17 cell differentiation at submicromolar concentrations. 2013-01-10 00:00:00 transcriptional activity Antagonizing ROR γt transcriptional activity receptor ROR γt submicromolar concentrations TH 17 cells ROR γ antagonists ROR γt Diphenylpropanamide 4 n TH 17 cell differentiation