Selective proteolysis represents a cutting-edge therapeutic approach that is garnering global interest due to its capacity to eradicate pathogenic biomolecules within cellular environments. For instance, the PROTAC technology brings the ubiquitin proteasome system degradation machinery in close proximity of the KRASG12D mutant protein for initiating its degradation and the clearing of abnormal protein debris with unparallel precision, which provides an edge over traditional protein inhibition. This Patent Highlight provides exemplary PROTAC compounds having activity as inhibitors or degraders of the G12D mutant KRAS protein.
Published 2023 by American Chemical Society.