January 1, 2025Open Access

Reductively Activated CPP-PROTAC Nanocomplexes Enhance Target Degradation via Efficient Cellular Uptake

Key Points

Enhancements in cellular uptake resulted in significantly greater BRD4 degradation in target cells.
The nanoparticle delivery system increased cellular uptake by utilizing a cell-penetrating peptide and a disulfide linker.
Development of this innovative delivery platform involved MZ1-R9 conjugation with dextran sulfate to improve efficacy.
This approach may enable more effective use of PROTAC technology for targeted cancer therapies.

Abstract

We developed a nanoparticle based on a cell-penetrating peptide-PROTAC conjugate with a disulfide linker, MZ1-R9, and dextran sulfate, enhancing cellular uptake and BRD4 degradation. This delivery platform significantly improves PROTAC...

Reductively Activated CPP-PROTAC Nanocomplexes Enhance Target Degradation via Efficient Cellular Uptake

Key Points

Abstract

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