Thiostrepton suppresses triple-negative breast cancer through downregulating c-FLIP/SMAD2/3 signaling pathway

J Asian Nat Prod Res. 2024 Aug;26(8):945-954. doi: 10.1080/10286020.2024.2343420. Epub 2024 Apr 18.

Abstract

Triple-negative breast cancer (TNBC) is an aggressive subtype with poor prognosis of breast cancer. Thiostrepton exerts anti-tumor activities against several cancers including TNBC. Herein we discussed the new molecular mechanisms of thiostrepton in TNBC. Thiostrepton inhibited MDA-MB-231 cell viability, accompanied by a decrease of c-FLIP and p-SMAD2/3. c-FLIP overexpression reduced the sensitivity of MDA-MB-231 cells to thiostrepton, while SMAD2/3 knockdown increased the sensitivity of MDA-MB-231 cells to thiostrepton. Moreover, c-FLIP overexpression significantly increased the expression and phosphorylation of SMAD2/3 proteins and vice versa. In conclusion, our study reveals c-FLIP/SMAD2/3 signaling pathway as a novel mechanism of antitumor activity of thiostrepton.

Keywords: SMAD2/3; Thiostrepton; c-FLIP; triple-negative breast cancer (TNBC).

MeSH terms

  • CASP8 and FADD-Like Apoptosis Regulating Protein / metabolism
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Down-Regulation / drug effects
  • Female
  • Humans
  • Molecular Structure
  • Signal Transduction* / drug effects
  • Smad2 Protein* / metabolism
  • Smad3 Protein* / metabolism
  • Triple Negative Breast Neoplasms* / drug therapy

Substances

  • Smad3 Protein
  • Smad2 Protein
  • CASP8 and FADD-Like Apoptosis Regulating Protein
  • SMAD2 protein, human
  • SMAD3 protein, human