E3 ligase Ligand-Linker Conjugates 9 是 E3 和 25 原子长度接头的配体偶联物。接头的接头是卤素基团。 E3 ligase Ligand-Linker Conjugates 9 包含基于 (S,R,S)-AHPC 的 VHL 配体和 6 单元 PEG 接头。 E3 ligase Ligand-Linker Conjugates 9 能够在基于细胞的分析中诱导 GFP-HaloTag7 的降解。
E3 ligase Ligand-Linker Conjugates 9 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
E3 ligase Ligand-Linker Conjugates 9 uses the VHL ligand[1]. The linker is 6-2-2-2-2-2-2. The linkers contain a mixture of hydrophobic and hydrophilic moieties to balance the hydrophobicity/hydrophilicity of the resulting hybrid compounds. PROTACs that induce the degradation of an oncogenic tyrosine kinase, BCR-ABL has been developed. E3 ligase Ligand-Linker Conjugates 9 can be attached to potent TKIs (bosutinib and dasatinib) that mediate the degradation of c-ABL and BCR-ABL by hijacking either CRBN or VHL E3 ubiquitin ligase [2].
[1]. US 20170121321 A1 [2]. Lai AC, et al. Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10.
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