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Cerulenin suppresses ErbB2-overexpressing breast cancer by targeting ErbB2/PKM2 pathway

Sinan Lv1, Yunwu Zhang1, Jiawei Song2

  • 1Department of Biochemistry and Molecular Biology, West China School of Basic Medical Sciences and Forensic Medicine, Sichuan University, No. 17, Section 3, South Renmin Road, Chengdu, 610041, China.

Medical Oncology (Northwood, London, England)
|October 29, 2022
PubMed

Insights

Cerulenin, a fatty acid synthase inhibitor, effectively suppresses proliferation, migration, invasion, and glycolysis in ErbB2-overexpressing breast cancer cells. It targets the ErbB2/PKM2 pathway, offering a potential new therapeutic strategy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • ErbB2-overexpressing breast cancer often develops treatment resistance.
  • Fatty acid synthase (FASN) inhibitors like cerulenin show anticancer potential.
  • The precise mechanisms of cerulenin's action in breast cancer require further elucidation.

Purpose of the Study:

  • To investigate cerulenin's effects on proliferation, migration, invasion, and glycolysis in ErbB2-overexpressing breast cancer cells.
  • To identify the molecular mechanisms underlying cerulenin's inhibitory actions.
  • To explore the potential role of PKM2 (pyruvate kinase M2) as a cerulenin target.

Main Methods:

  • Bioinformatic analysis to identify potential molecular targets.
  • Cell-based assays to assess proliferation, migration, invasion, and glycolysis.
  • Western blot analysis to evaluate protein expression levels (ErbB2, PKM2, EMT markers).
  • Rescue experiments by replenishing PKM2.

Main Results:

  • Cerulenin significantly inhibited proliferation, migration, invasion, and glycolysis in ErbB2-overexpressing breast cancer cells.
  • Bioinformatic analysis suggested PKM2 as a target of cerulenin.
  • Cerulenin downregulated ErbB2, PKM2, and epithelial-mesenchymal transition (EMT) markers (MMP9, MMP2, Snail2) in a dose- and time-dependent manner.
  • PKM2 replenishment rescued the inhibitory effects of cerulenin.

Conclusions:

  • Cerulenin exerts its inhibitory effects on ErbB2-overexpressing breast cancer by targeting the ErbB2/PKM2 pathway.
  • Cerulenin effectively suppresses key malignant phenotypes including proliferation, migration, invasion, and glycolysis.
  • This study highlights cerulenin as a promising therapeutic agent for ErbB2-overexpressing breast cancer.
Keywords:
Breast cancerCeruleninErbB2PKM2

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