Targeted degradation of EGFR 19Del by PROTACs suppresses tumor growth in non-small-cell lung cancer.

ABSTRACT:

Object

The occurrence of acquired resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) poses a significant challenge in treating non-small-cell lung cancer (NSCLC), limiting the clinical use of EGFR-TKIs. Proteolysis-targeting chimeras (PROTACs) demonstrate promise in preclinical settings. This study is aimed to design effective EGFR degraders by linking CRBN ligands with relatively lower molecular weights.

Methods

Computational methods are employed to do the rational design for the PROTACs. Western blots are used to examine the expression of proteins including EGFR. Cell viability and colony-formation assays are conducted to evaluate the anti-proliferative effects of degraders to NSCLC cell lines, and apoptosis assays are assessed by Annex

SUBMITTER: Piao L 

PROVIDER: S-EPMC12592173 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature