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