Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506-Binding Protein 51 (FKBP51),Angewandte Chemie International Edition

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Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506-Binding Protein 51 (FKBP51)
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2023-11-09 , DOI: 10.1002/anie.202309706
Thomas M Geiger ₁ , Michael Walz ₁ , Christian Meyners ₁ , Angela Kuehn ₁ , Johannes K Dreizler ₁ , Wisely O Sugiarto ₁ , Edvaldo V S Maciel ₁ , Min Zheng ₁ , Frederik Lermyte ₁ , Felix Hausch _{1,

2}

Affiliation

The FK506-binding site of FK506-binding protein 51 (FKBP51) is chemically tractable but not required for glucocorticoid receptor (GR) repression by FKBP51. The proteolysis targeting chimera SelDeg51 enables degradation of FKBP51, abolishes its scaffolding functions, and reactivates GR signaling.

中文翻译：

发现一种针对嵌合体的有效蛋白水解作用，能够靶向 FK506 结合蛋白 51 (FKBP51) 的支架功能

FK506 结合蛋白 51 (FKBP51) 的 FK506 结合位点在化学上易于处理，但不是 FKBP51 抑制糖皮质激素受体 (GR) 所必需的。针对嵌合体 SelDeg51 的蛋白水解作用能够降解 FKBP51，消除其支架功能，并重新激活 GR 信号传导。

更新日期：2023-11-09

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