Work at Blueprint Medicines Corp. to identify a selective and potent CDK4 degrader led to the identification of BLU-448, with minimal activity against CDK6 for treating HR+/HER2- breast cancer.
Foghorn Therapeutics Inc. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding agent coupled to a histone acetyltransferase p300 (EP300)-targeting moiety. As such, they are described as EP300 degradation inducers potentially useful for the treatment of cancer.