Targeting TRAF6/IRF3 axis to inhibit NF-κB-p65 nuclear translocation enhances the chemosensitivity of 5-FU and reverses the proliferation of gastric cancer

Cell Death Dis. 2024 Dec 20;15(12):924. doi: 10.1038/s41419-024-07290-5.

Abstract

Chemoresistance poses a significant clinical challenge in the treatment of gastric cancer (GC), while its underlying molecular mechanisms are still not fully understood. Post-translational protein modification and abnormal activation of nuclear factor-kappa B (NF-κB) are critical regulators of tumor chemoresistance. This study investigates the role of TNF receptors-associated factors 6 (TRAF6) in 5-Fluorouracil (5-FU) resistant GC. Utilizing short hairpin RNA (shRNA) to suppress TRAF6 expression in 5-FU resistant GC cells across both in vivo and in vitro models, we observed a marked reduction in cell proliferation and tumor growth. Low expression of TRAF6 inhibited nuclear translocation of NF-κB-p65, which was achieved by promoting the expression of Interferon regulatory factor 3 (IRF3). Importantly, TRAF6, an E3 ubiquitin ligase, bound to the IRF3-Δ (SR + IAD) (1-190aa) domain, inducing Lys70 ubiquitination of IRF3 to regulate its protein stability, with ubiquitin K48 residue playing a crucial role in this process. In conclusion, our study reveals the mechanism by which the TRAF6/IRF3 axis decreases GC's cells sensitivity to 5-FU by promoting nuclear translocation of NF-κB-p65, offering valuable insights into overcoming chemoresistance in GC.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Nucleus / metabolism
  • Cell Proliferation* / drug effects
  • Drug Resistance, Neoplasm* / drug effects
  • Fluorouracil* / pharmacology
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Interferon Regulatory Factor-3* / metabolism
  • Intracellular Signaling Peptides and Proteins
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Signal Transduction / drug effects
  • Stomach Neoplasms* / drug therapy
  • Stomach Neoplasms* / genetics
  • Stomach Neoplasms* / metabolism
  • Stomach Neoplasms* / pathology
  • TNF Receptor-Associated Factor 6* / metabolism
  • Transcription Factor RelA* / metabolism
  • Ubiquitination

Substances

  • Fluorouracil
  • TNF Receptor-Associated Factor 6
  • Interferon Regulatory Factor-3
  • Transcription Factor RelA
  • IRF3 protein, human
  • Tifab protein, human
  • Intracellular Signaling Peptides and Proteins