Targeting G9a Exerts Pleiotropic Suppression in Triple-Negative Breast Cancer Cells: Cooperatively Inducing

Jialin Li1, Guijuan Zhang2, Tianyang Liu3

  • 1The First School of Clinical Medicine, State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, Jinan University, Guangzhou 510632, China.

Biomolecules
|March 28, 2026
PubMed

Insights

Inhibiting G9a suppresses triple-negative breast cancer (TNBC) by triggering pyroptosis, a programmed cell death. This occurs through the RIG-I/STAT1/GSDME pathway, offering a new therapeutic strategy for TNBC.

Area of Science:

  • Oncology
  • Cell Biology
  • Molecular Biology

Background:

  • Pyroptosis, a pro-inflammatory programmed cell death, is crucial in tumor biology, particularly in triple-negative breast cancer (TNBC).
  • G9a inhibition shows anticancer potential, but its precise molecular mechanisms in TNBC remain largely unelucidated.
  • Understanding these mechanisms is vital for developing novel therapeutic strategies against TNBC.

Purpose of the Study:

  • To investigate whether G9a inhibition suppresses TNBC progression by promoting pyroptosis.
  • To elucidate the molecular pathways involved in G9a inhibition-induced pyroptosis in TNBC cells.

Main Methods:

  • Utilized TNBC cell lines (MDA-MB-231, SUM159PT) and a normal cell line (MCF-10A) for in vitro studies.
  • Assessed cell proliferation, death, invasion, and migration using CCK8, EdU, flow cytometry, and transwell assays.
  • Analyzed inflammatory factors, gene/protein expression (RIG-I, STAT1, GSDME), and cellular morphology via ELISA, qRT-PCR, Western blot, immunofluorescence, and transmission electron microscopy.

Main Results:

  • G9a knockdown significantly inhibited TNBC cell growth, invasion, and migration.
  • G9a inhibition induced pyroptosis and upregulated RIG-I, p-STAT1, and GSDME expression in TNBC cells.
  • RIG-I inhibition partially reversed the pyroptosis induced by G9a knockdown, confirming the pathway's role.

Conclusions:

  • G9a inhibition triggers pyroptosis in TNBC cells via the RIG-I/STAT1/GSDME signaling pathway.
  • This pathway presents a novel therapeutic target for treating triple-negative breast cancer.
  • Targeting G9a offers a promising strategy for enhancing anti-TNBC treatment efficacy.

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