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Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.

ABSTRACT: Retinoic acid-related orphan receptor RORγt plays a pivotal role in the differentiation of T_H17 cells. Antagonizing RORγt transcriptional activity is a potential means to treat T_H17-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 T_H17 cell differentiation at sub-micromolar concentrations.

SUBMITTER: Huh JR

PROVIDER: S-EPMC3770298 | biostudies-literature |

REPOSITORIES: biostudies-literature

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