NIH R01 · 2024
Optimizing PepTAC structure and amphiphilicity for enhanced target protein degradation
Project Summary This study seeks to advance heterobifunctional degraders that induce targeted protein degradation through the ubiquitin proteasome pathway. Typically, molecular degraders involve a ligand that recruits an E3 ubiquitin ligase and another that targets a protein of interest (POI), forming an E3:Degrader:POI ternary complex, leading to POI ubiquitination and subsequent degradation by the 26S proteasome. Peptide-based proteolysis targeting chimeras (PepTACs) offer distinct advantages over small molecule degraders for targeting protein-protein interactions due to their specificity, manufacturability, ease of design, and expansive binding surface area. However, due to challenges…
From the public funding record at NIH RePORTER. Describes the funded project, not the reviews below.