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Papers of the Week


Papers: 18 Mar 2023 - 24 Mar 2023

RESEARCH TYPE:
Review


Pharmacology/Drug Development

PAIN TYPE:
Psychological/Comorbidities


2023 Mar 10


ACS Pharmacol Transl Sci


36926456


6


3

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

Authors

Buffa V, Knaup FH, Heymann T, Springer M, Schmidt MV, Hausch F

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.