A Structural Explanation of the Effects of Dissociated Glucocorticoids on Glucocorticoid Receptor Transactivation

  title={A Structural Explanation of the Effects of Dissociated Glucocorticoids on Glucocorticoid Receptor Transactivation},
  author={Xavier Dezitter and J{\'e}r{\^o}me Fagart and Solenne Taront and Michèle Fay and Bernadette Masselot and Dominique H{\'e}tuin and Pierre Formstecher and Marie-Edith Rafestin-Oblin and Thierry Idziorek},
  journal={Molecular Pharmacology},
  pages={226 - 236}
There is a therapeutic need for glucocorticoid receptor (GR) ligands that distinguish between the transrepression and transactivation activity of the GR, the later thought to be responsible for side effects. These ligands are known as “dissociated glucocorticoids” (dGCs). The first published dGCs, RU24782 (9α-fluoro-11β-hydroxy-16α-methylpregna-21-thiomethyl-1,4-diene-3,20-dione) and RU24858 (9α-fluoro-11β-hydroxy-16α-methylpregna-21-cyanide-1,4-diene-3,20-dione), do not have the 17α-hydroxyl… 

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