title: Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.
abstract: 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. Diphenylpropanamide4ninhibited transcriptional activity of RORγt, but not RORα, in cells. In addition, it suppressed human TH17 cell differentiation at sub-micromolar concentrations.
authors.affiliation: Molecular Pathogenesis Program, The Kimmel Center for Biology and Medicine of the Skirball Institute, New York University School of Medicine, New York, NY 10016, USA.
authors.forename: Jun R
authors.initials: JR
authors.lastname: Huh
authors.forename: Erika E
authors.initials: EE
authors.lastname: Englund
authors.forename: Hang
authors.initials: H
authors.lastname: Wang
authors.forename: Ruili
authors.initials: R
authors.lastname: Huang
authors.forename: Pengxiang
authors.initials: P
authors.lastname: Huang
authors.forename: Fraydoon
authors.initials: F
authors.lastname: Rastinejad
authors.forename: James
authors.initials: J
authors.lastname: Inglese
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Austin
authors.forename: Ronald L
authors.initials: RL
authors.lastname: Johnson
authors.forename: Wenwei
authors.initials: W
authors.lastname: Huang
authors.forename: Dan R
authors.initials: DR
authors.lastname: Littman
keywords: RORγ antagonist; Retinoic acid-related orphan receptor; TH17-related autoimmune diseases; diphenylpropanamide
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