Document Report Card

ID: ALA2321802

Journal: ACS Med Chem Lett

Title: Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.

Authors: Huh JR, Englund EE, Wang H, Huang R, Huang P, Rastinejad F, Inglese J, Austin CP, Johnson RL, Huang W, Littman DR.

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. Diphenylpropanamide 4n inhibited transcriptional activity of RORγt, but not RORα, in cells. In addition, it suppressed human TH17 cell differentiation at sub-micromolar concentrations.

CiteXplore: 24040486

DOI: 10.1021/ml300286h