Development of PROTACS degrading KRAS and SOS1
Gerhard Hamilton, Marie-Therese Eggerstorfer, Sandra Stickler
2024Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics13 citationsDOIOpen Access PDF
Abstract
compared to their cognate inhibitors but their toxicity in normal tissues is not clear. The CRBN PROTACs containing thalidomide derivatives cannot be tested in experimental animals. Resistance to such PROTACS arises through downregulation or inactivation of CRBN or factors of the functional VHL E3 ubiquitin ligase. Although highly active KRAS and SOS1 PROTACs have been formulated their clinical application remains difficult.
Topics & Concepts
KRASChemistryComputational biologyBiologyBiochemistryMutationGeneProtein Degradation and InhibitorsNeuroblastoma Research and TreatmentsPeptidase Inhibition and Analysis