Proteolysis Targeting Chimeras (PROTACs) Based on Imatinib Induced Degradation of BCR-ABL in K562 Cells,ChemistrySelect

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Proteolysis Targeting Chimeras (PROTACs) Based on Imatinib Induced Degradation of BCR-ABL in K562 Cells
ChemistrySelect ( IF 1.9 ) Pub Date : 2023-04-14 , DOI: 10.1002/slct.202300095
Chuang Li ₁ , Peng Zhang ₂ , Gaojie Chang ₁ , Mingyue Pan ₂ , Fengke Lu ₁ , Jiahao Huang ₁ , Yanzhi Wang ₁ , Qingyan Zhao ₁ , Bingxia Sun ₁ , Yuting Cui ₁ , Feng Sang ₁

Affiliation

Fifteen new proteolysis targeting chimeras (PROTACs) based on Imatinib and Thalidomide have been designed, synthesized, and evaluated for their antiproliferative activity against K562 cells. PROTAC with a 2-oxoethyl linker exhibited significant activity against K562 cells (IC₅₀=0.62±0.02 μM). Western blot results showed that the new PROTAC reduced the level of BCR-ABL through ubiquitin-proteasome system (UPS) pathway.

中文翻译：

基于伊马替尼诱导 K562 细胞 BCR-ABL 降解的蛋白水解靶向嵌合体 (PROTAC)

已经设计、合成了 15 种基于伊马替尼和沙利度胺的新型蛋白水解靶向嵌合体 (PROTAC)，并评估了它们对 K562 细胞的抗增殖活性。具有 2-氧代乙基接头的 PROTAC 对 K562 细胞表现出显着的活性（IC ₅₀ =0.62±0.02 μM）。蛋白质印迹结果表明，新的 PROTAC 通过泛素-蛋白酶体系统 (UPS) 途径降低了 BCR-ABL 的水平。

更新日期：2023-04-16

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