Proteolysis targeting chimeras in non-small cell lung cancer
Garo Hagopian, Christopher H. Grant, Misako Nagasaka
Abstract
Non-small cell lung cancer (NSCLC) has very poor prognosis in advanced stages. Discovery and application of therapies targeting specific oncogenic driver mutations has greatly improved overall survival. However, targeted therapies are limited in their efficacy due to resistance mutations that may arise with long term use. Proteolysis targeting Chimeras (PROTACs) are a promising approach to combating resistance mutations. PROTACs commandeer innate ubiquitination machinery to degrade oncogenic proteins. Here we review the PROTACs that have been developed for targeting common EGFR, KRAS, and ALK mutations.
Topics & Concepts
MedicineKRASLung cancerCancer researchCancerTargeted therapyOncologyInternal medicineColorectal cancerProtein Degradation and InhibitorsPeptidase Inhibition and AnalysisUbiquitin and proteasome pathways