Radiation responsive PROTAC nanoparticles for tumor-specific proteolysis enhanced radiotherapy

Abstract

Proteolysis targeting chimeras (PROTACs) is a promising strategy for cancer therapy. However, the always-on bioactivity of PROTACs may lead to non-target toxicity which restrict their antitumor performance. Here, we developed...

A photoactivatable upconverting nanodevice boosts the lysosomal escape of PROTAC degraders for enhanced combination therapy

“…Proteolysis Targeting Chimeras (PROTACs) have revolutionized the field of targeted therapy by utilizing the ubiquitin-proteasome system (UPS) to selectively degrade disease-related proteins. 1–3 These heterobifunctional molecules function by recruiting an E3 ubiquitin ligase to tag the protein of interest (POI) for degradation, offering a highly specific approach compared to traditional small-molecule inhibitors. 4,5 Despite their efficacy, the clinical application of conventional PROTACs is hindered by issues such as “on-target, off-tumor” toxicity and limitations in delivery and controlled release.…”