2. Academic Validation
  3. Identification of Potent and Selective RORγ Antagonists

Identification of Potent and Selective RORγ Antagonists

Wenwei Huang 1,  Hang Wang 1,  Ronald L. Johnson 1,  Ruili Huang 1,  Erika E. Englund 1,  Jun Huh 2,  Dan R. Littman 2
Affiliations

Affiliations

  • 1 NIH Chemical Genomics Center, NIH Center for Translational Therapeutics,NIH Chemical Genomics Center, National Human Genome Research Institute, NationalInstitutes of Health, Rockville, MD.
  • 2 Skirball Institute of Biomolecular Medicine, New York University, NewYork, NY.
PMID: 23658948
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. In this report, we present the identification of a series of diphenylpropanamides as novel and selective RORγt antagonists. ML209 inhibited transcriptional activity of RORγt, but not RORα, in cells. In addition, it suppressed Th17 cell differentiation at submicromolar concentrations.

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