Potent PROTACs Targeting EGFR Mutants in Drug Discovery.

Epidermal growth factor receptor (EGFR) upregulations are found in many types of cancers, including breast cancer, cholangiocarcinoma, ovarian cancer, prostate cancer, leukemia, and colon cancer. This Patent Highlight showcases PROTAC compounds formed by conjugating EGFR inhibitor with E3 ligase ligand, which recruit targeted proteins to E3 ubiquitin ligase for EGFR mutant protein degradation.