Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the 
FK506-Binding Protein 51

Buffa, Vanessa; Knaup, Fabian H.; Heymann, Tim; Springer, Margherita; Schmidt, Mathias V.; Hausch, Felix

doi:10.1021/acsptsci.2c00234

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Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51

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Springer, Margherita
RG Stress Resilience, Max Planck Institute of Psychiatry, Max Planck Society;

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Schmidt, Mathias V.
RG Stress Resilience, Max Planck Institute of Psychiatry, Max Planck Society;

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Citation

Buffa, V., Knaup, F. H., Heymann, T., Springer, M., Schmidt, M. V., & Hausch, F. (2023). Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51. ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE. doi:10.1021/acsptsci.2c00234.

Cite as: https://hdl.handle.net/21.11116/0000-000D-037C-5

Abstract

The FK506-binding protein 51 (FKBP51) has emerged as an important regulator of the mammalian stress response and is involved in persistent pain states and metabolic pathways. The FK506 analog SAFit2 (short for selective antagonist of FKBP51 by induced fit) was the first potent and selective FKBP51 ligand with an acceptable pharmacokinetic profile. At present, SAFit2 represents the gold standard for FKBP51 pharmacology and has been extensively used in numerous biological studies. Here we review the current knowledge on SAFit2 as well as guidelines for its use.