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Updated: Oct 20, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
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Published on: November 9, 2020

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標的型タンパク質分解のためのE3リガゼKEAP1の活用

Jieli Wei1, Fanye Meng1, Kwang-Su Park1

  • 1Mount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.

Journal of the American Chemical Society
|September 14, 2021
PubMed
まとめ

この研究では,標的型タンパク質分解のためにKEAP1 E3リガスを用いた新しいタンパク質分解標的化キメラ (PROTAC) が導入されています. 新しいPROTAC,MS83は,BRD4とBRD3のタンパク質を効果的に分解し,耐久性と抗増殖活性性を高めます.

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