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Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

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
Summary

This study introduces a novel Proteolysis Targeting Chimera (PROTAC) using the KEAP1 E3 ligase for targeted protein degradation. The new PROTAC, MS83, effectively degrades BRD4 and BRD3 proteins with enhanced durability and antiproliferative activity.

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