Targeted polymeric nanoparticles enable epithelial translocation of PROTACs and preserve intracellular protein degradation activity
Abstract
Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality for the degradation of disease-associated proteins. Despite their high therapeutic potential, their clinical translation is limited by poor membrane permeability and low oral bioavailability resulting from their beyond-rule-of-five physicochemical properties. Here, we report a targeted nanoparticle-based delivery strategy designed to facilitate intestinal permeation while preserving degradation efficiency in target cells. The CA19-9 antibody 121SLE was covalently coupled to the surface of PROTAC-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (hydrodynamic diameter
Fields of Study & Subjects
Protein Degradation and Inhibitors
Click Chemistry and Applications
Peptidase Inhibition and Analysis
Publication details
- Journal / source
- European Journal of Pharmaceutical Sciences
- Publisher
- Elsevier BV
- Volume
- 224
- Pages
- 107587–107587
- Publication date
- 14 June 2026
- Language
- EN