Identification of Potent
and Selective Diphenylpropanamide
RORγ Inhibitors
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Abstract
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
