Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms.

@article{Xiao2014SmallmoleculeRA,
  title={Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms.},
  author={Sheng Xiao and Nir Yosef and Jianfei Yang and Yonghui Wang and L Zhou and Chen Zhu and Chuan Wu and Erkan Baloglu and Darby Schmidt and Radha Ramesh and Mercedes Lobera and Mark S. Sundrud and Pei-Yun Tsai and Zhijun Xiang and Jinsong Wang and Yan Xu and Xichen Lin and Karsten Kretschmer and Peter B. Rahl and Richard A. Young and Zhong Zhong and David A. Hafler and Aviv Regev and Shomir Ghosh and Alexander Marson and Vijay K Kuchroo},
  journal={Immunity},
  year={2014},
  volume={40 4},
  pages={477-89}
}
We identified three retinoid-related orphan receptor gamma t (RORγt)-specific inhibitors that suppress T helper 17 (Th17) cell responses, including Th17-cell-mediated autoimmune disease. We systemically characterized RORγt binding in the presence and absence of drugs with corresponding whole-genome transcriptome sequencing. RORγt acts as a direct activator of Th17 cell signature genes and a direct repressor of signature genes from other T cell lineages; its strongest transcriptional effects are… CONTINUE READING

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