Thalidomide and its derivatives are the only protein degraders currently used in clinical practice. This tutorial review provides an overview of the mechanism of action of thalidomide-based degraders and their future perspectives.
This review comprehensively illustrates chemistries of E3 ligase ligands, which were used successfully in the development of PROTACs.
This study enables rapid synthesis of pomalidomide-conjugates for PROTACs by optimizing temperature and reagent addition, reducing reaction time to minutes with fewer byproducts, and improving efficiency and sustainability in drug development.
The fluorescent properties of pomalidomide derivatives have been utilised to develop a high-throughput imaging method suitable for rapid screening of protein degrader candidates.
In this study, we discovered 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O’PROTAC for ERG destruction, expanding the pool of ligands for development of PROTACs, especially O’PROTACs.