选择性拮抗剂SAFit2作为FK506结合蛋白51化学探针的分析
Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51.
作者信息
Buffa Vanessa, Knaup Fabian H, Heymann Tim, Springer Margherita, Schmidt Mathias V, Hausch Felix
机构信息
Department of Chemistry and Biochemistry, Clemens-Schöpf-Institute, Technical University Darmstadt, Alarich-Weiss Straße 4, 64287 Darmstadt, Germany.
Research Group Neurobiology of Stress Resilience, Max Planck Institute of Psychiatry, 80804 Munich, Germany.
出版信息
ACS Pharmacol Transl Sci. 2023 Feb 14;6(3):361-371. doi: 10.1021/acsptsci.2c00234. eCollection 2023 Mar 10.
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.
摘要
FK506结合蛋白51（FKBP51）已成为哺乳动物应激反应的重要调节因子，并参与持续性疼痛状态和代谢途径。FK506类似物SAFit2（诱导契合作用下FKBP51的选择性拮抗剂的缩写）是首个具有可接受药代动力学特征的强效且选择性的FKBP51配体。目前，SAFit2代表了FKBP51药理学的金标准，并已广泛应用于众多生物学研究中。在此，我们综述了关于SAFit2的现有知识及其使用指南。
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