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

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.

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Item Permalink: https://hdl.handle.net/21.11116/0000-000D-037C-5 Version Permalink: https://hdl.handle.net/21.11116/0000-000D-037D-4

Genre: Book Review

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Buffa, Vanessa, Author
Knaup, Fabian H., Author
Heymann, Tim, Author
Springer, Margherita¹, Author
Schmidt, Mathias V.¹, Author
Hausch, Felix, Author

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1RG Stress Resilience, Max Planck Institute of Psychiatry, Max Planck Society, ou_2040294

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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.

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Dates: Published Online: 2023

Publication Status: Published online

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Identifiers: ISI: 000933936800001
DOI: 10.1021/acsptsci.2c00234

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Title: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

Source Genre: Journal

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