Article
Selective inhibitors of the FK506-binding protein 51 by induced fit.
Nature chemical biology - 1 Jan 2015
Gaali Steffen, Kirschner Alexander, Cuboni Serena, Hartmann Jakob, Kozany Christian, Balsevich Georgia, Namendorf Christian, Fernandez-Vizarra Paula, Sippel Claudia, Zannas Anthony S, Draenert Rika, Binder Elisabeth B, Almeida Osborne F X, Rühter Gerd, Uhr Manfred, Schmidt Mathias V, Touma Chadi, Bracher Andreas, Hausch Felix
Abstract excerpt
The FK506-binding protein 51 (FKBP51, encoded by the FKBP5 gene) is an established risk factor for stress-related psychiatric disorders such as major depression. Drug discovery for FKBP51 has been hampered by the inability to pharmacologically differentiate against the structurally similar but functional opposing homolog FKBP52, and all known FKBP ligands are unselective. Here, we report the discovery of the...
Topics
- Adaptation, Psychological
- Animals
- Antidepressive Agents
- Behavior, Animal
- Binding Sites
- Cells, Cultured
- Drug Discovery
- Humans
- Male