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1,1,1-Trifluoroethyl-PEG4-azide 是一种含有叠氮基和三氟乙基的交联剂。叠氮基可以参与与炔烃、DBCO 和 BCN 等试剂的点击化学反应。PEG 修饰增加了所得化合物的水溶性。三氟乙基被认为是一种酰胺等排物,用于与蛋白质、抗体和其他分子和表面中的赖氨酸和其他伯胺基团相互作用。
1,1,1-Trifluoroethyl-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
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