Potent PROTACs Targeting EGFR Mutants in Drug Discovery
Robert B. Kargbo
Abstract
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.
Topics & Concepts
Ubiquitin ligaseEpidermal growth factor receptorDrug discoveryCancer researchMutantCancerDrugEGFR inhibitorsUbiquitinMedicineBioinformaticsChemistryBiologyPharmacologyInternal medicineBiochemistryGeneProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis