Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.

@article{Miner2007AntiinflammatoryGR,
  title={Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.},
  author={Jeffrey N. Miner and Bob Ardecky and Khalid Benbatoul and K. D. Griffiths and Christopher J. Larson and Dale E. Mais and Keith Marschke and Jon Rosen and Eric G Vajda and Lin Zhi and Andr{\'e}s Negro-Vilar},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2007},
  volume={104 49},
  pages={19244-9}
}
Glucocorticoids are commonly used antiinflammatory agents whose use is limited by side effects. We have developed a series of glucocorticoid receptor (GR) ligands that retain the strong antiinflammatory activity of conventional glucocorticoids with reduced side effects. We present a compound, LGD5552, that binds the receptor efficiently and strongly represses inflammatory gene expression. LGD5552 bound to GR activates gene expression somewhat differently than glucocorticoids. It activates some… CONTINUE READING