Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead

This is the authors' abstract. We don't add key points for this paper.

, and in cells the BRD4 degrader is insensitive to wash-out and competition by potent reversible CRBN ligands, reflecting enhanced pharmacodynamics. We anticipate that covalent CRBN-based PROTACs will enhance degradation efficiencies, thus expanding the scope of addressable targets using the heterobifunctional degrader modality.