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

被引：11

作者：

Buffa, Vanessa ^{[1
]}

Knaup, Fabian H. ^{[1
]}

Heymann, Tim ^{[1
]}

Springer, Margherita ^{[2
]}

Schmidt, Mathias V. ^{[2
]}

Hausch, Felix ^{[1
]}

机构：

[1] Tech Univ Darmstadt, Clemens Schopf Inst, Dept Chem & Biochem, D-64287 Darmstadt, Germany

[2] Max Planck Inst Psychiat, Res Grp Neurobiol Stress Resilience, D-80804 Munich, Germany

来源：

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE | 2023年

关键词：

SAFit2; FKBP51; chemical tools; transient binding pockets; GLUCOCORTICOID-RECEPTOR; IMMUNOPHILIN FKBP51; SIGNALING PATHWAY; STRESS; LIGANDS; ASSOCIATION; EXPLORATION; EXPRESSION; INHIBITOR; SCAFFOLD;

D O I：

10.1021/acsptsci.2c00234

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：361 / 371

页数：11

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