Discovery of novel Keap1-targeting hydrophobic tag (HyT) tethering degraders with potent Nrf2 activation activity

Key Points

• Hydrophobic tag tethering degraders show significant Nrf2 activation effects, indicating strong potential for therapeutic applications.
• Nrf2 activation was notably enhanced by these novel degraders, achieving a marked increase in activity levels.
• Comprehensive analysis of Keap1-targeting mechanisms highlights the efficiency of these degraders in cellular models.
• Potential for novel therapeutic strategies emerges, though current findings require further validation in clinical settings.