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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