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A Combined 3D Tissue Engineered In Vitro/In Silico Lung Tumor Model for Predicting Drug Effectiveness in Specific Mutational Backgrounds
Published on: April 6, 2016
EIF4E promotes gefitinib resistance in non-small cell lung cancer by activating the Wnt/β-catenin pathway
Bo Zhang1,2, Jiani Zhu3, Zixian Jin1
1Department of Thoracic Surgery, Taizhou Hospital of Zhejiang Province Affiliated to Wenzhou Medical University, Linhai, Zhejiang, China.
Abstract:
Tyrosine kinase inhibitors (TKIs) like gefitinib, which target the epidermal growth factor receptor (EGFR), show considerable therapeutic effectiveness in non-small cell lung cancer (NSCLC) with EGFR-activating mutations. Nevertheless, the resistance that develops against EGFR-TKIs diminishes their therapeutic impact in clinical settings. This investigation focused on the impact of eukaryotic translation initiation factor 4E (eIF4E) on gefitinib resistance in NSCLC. Using the CCK-8 assay, the influence of different gefitinib concentrations on cell proliferation was examined. eIF4E and EGFR expressions were verified by qRT-PCR and/or western blotting in NSCLC cell lines. Moreover, the effects of eIF4E knockdown in gefitinib-treated PC9/GR cells were detected by CCK-8, flow cytometry, colony formation assays, and xenograft tumor model. eIF4E expression was remarkably upregulated in the gefitinib-resistant PC9/GR cells. Moreover, the expression levels of eIF4E in NSCLC cell lines exhibited a dose-dependent increase following gefitinib administration. The function assays demonstrated that reducing eIF4E levels hindered the proliferation of PC9/GR cells and enhanced the apoptosis-inducing effects of gefitinib both in vitro and in vivo, and also had an inhibitory action on the Wnt/β-catenin pathway. Taken together, these results suggested that eIF4E confers gefitinib resistance in NSCLC by regulating the Wnt/β-catenin pathway. Therefore, eIF4E is a possible therapeutic target for improving therapeutic action in NSCLC patients who have developed resistance to gefitinib.
Insights
Eukaryotic translation initiation factor 4E (eIF4E) promotes gefitinib resistance in non-small cell lung cancer (NSCLC). Targeting eIF4E may overcome resistance and improve treatment outcomes for NSCLC patients.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Research
Background:
- Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) like gefitinib are effective for non-small cell lung cancer (NSCLC) with activating mutations.
- Acquired resistance to EGFR-TKIs is a major clinical challenge, limiting long-term patient benefit.
Purpose of the Study:
- To investigate the role of eukaryotic translation initiation factor 4E (eIF4E) in gefitinib resistance in NSCLC.
- To explore eIF4E as a potential therapeutic target to overcome gefitinib resistance.
Main Methods:
- CCK-8 assays to assess cell proliferation and gefitinib sensitivity.
- Quantitative reverse transcription PCR (qRT-PCR) and western blotting to measure eIF4E and EGFR expression.
- Functional assays including flow cytometry and colony formation assays after eIF4E knockdown.
- In vivo studies using a xenograft tumor model.
Main Results:
- eIF4E expression was significantly upregulated in gefitinib-resistant NSCLC cells (PC9/GR) and increased dose-dependently with gefitinib treatment.
- Knockdown of eIF4E inhibited proliferation, enhanced gefitinib-induced apoptosis in PC9/GR cells in vitro and in vivo.
- eIF4E inhibition suppressed the Wnt/β-catenin pathway.
Conclusions:
- eIF4E plays a crucial role in conferring gefitinib resistance in NSCLC.
- eIF4E mediates resistance by regulating the Wnt/β-catenin pathway.
- Targeting eIF4E represents a promising strategy to overcome gefitinib resistance in NSCLC.
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