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Selective inhibitors of the FK506-binding protein 51 by induced fit.
TLDR
It is demonstrated that selective inhibition of FKBP51 enhances neurite elongation in neuronal cultures and improves neuroendocrine feedback and stress-coping behavior in mice, providing the structural and functional basis for the development of mechanistically new antidepressants. Expand
Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties
TLDR
This is the first in vivo study using a specific FK BP51 antagonist, thereby unraveling the role of FKBP51 and its potential as a novel drug target for the improved treatment of anxiety-related disorders. Expand
Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
TLDR
This work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51. Expand
Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs).
TLDR
To create highly efficient inhibitors for FK506-binding proteins, a new asymmetric synthesis for pro-(S)-C(5) -branched aza-amide bicycles was developed, which resulted in novel protein contacts with the psychiatric risk factor FKBP51, which led to a more than 280-fold enhancement in affinity. Expand
Rationales Design und asymmetrische Synthese potenter neuritotropher Liganden für FK506‐bindende Proteine (FKBPs)
Um hochst effiziente Inhibitoren fur FK506-bindende Proteine zu erzielen, wurde eine neue asymmetrische Synthese fur pro-(S)-C5-verzweigte [4.3.1]-Aza-Amid-Bicyclen entwickelt. Der entscheidendeExpand
Mechanosensitive channel inhibition attenuates TGFβ2-induced actin cytoskeletal remodeling and reactivity in mouse optic nerve head astrocytes
TLDR
The data suggest inhibition of mechanosensitive channel activity as a potential therapeutic strategy to modulate actin cytoskeletal remodeling within the optic nerve head in glaucoma. Expand
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