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Inhibition of the AT-Hook DNA-Binding Domain Attenuates HMGA2-Mediated Epithelial Mesenchyme Transition in Esophageal

Lucas de Jesus Lima1, Matheus Lohan-Codeço1, Maria Luísa Barambo Wagner1

  • 1Laboratório de Interações Celulares, Instituto de Ciências Biomédicas, Programa de Pesquisa em Biologia Celular e do Desenvolvimento, Universidade Federal do Rio de Janeiro, Prédio do Centro de Ciências da Saúde-Cidade Universitária, Ilha do Fundão, Rua César Pernetta, 1766 (LS.3.01), Rio de Janeiro 21941-902, Brazil.

International Journal of Molecular Sciences
|August 13, 2026
PubMed

Insights

Blocking HMGA2-DNA interactions with netropsin inhibits esophageal squamous cell carcinoma (ESCC) progression. This approach reduces cell viability, migration, and EMT, while enhancing apoptosis and sensitizing cells to chemotherapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Therapeutics

Background:

  • Esophageal squamous cell carcinoma (ESCC) is a prevalent cancer with limited treatment options due to poor molecular characterization.
  • HMGA proteins, overexpressed in tumors, are potential therapeutic targets due to their role in regulating genes associated with tumor progression.
  • Targeting HMGA2-DNA interactions offers a novel strategy for ESCC treatment.

Purpose of the Study:

  • To investigate the effects of blocking HMGA2-DNA interactions using netropsin on ESCC progression.
  • To evaluate netropsin's impact on cell viability, migration, cell cycle, apoptosis, and Epithelial-Mesenchymal Transition (EMT).
  • To assess the potential of netropsin in combination with 5-Fluorouracil chemotherapy.

Main Methods:

  • In silico, translational, and in vitro approaches were employed.
  • Netropsin, an AT-hook DNA-binding ligand, was used to block HMGA2-DNA interactions.
  • Cell viability, migration, cell cycle, apoptosis, EMT markers (Slug, Twist), and response to 5-Fluorouracil were analyzed.

Main Results:

  • Netropsin significantly reduced ESCC cell viability, migration, and cell cycle progression.
  • Netropsin treatment promoted apoptosis in ESCC cells.
  • Netropsin partially reverted EMT activation by downregulating Slug and Twist, and sensitized ESCC cells to 5-Fluorouracil.

Conclusions:

  • Blocking HMGA2-DNA interactions with netropsin is a promising strategy for inhibiting ESCC progression.
  • Netropsin demonstrates anti-cancer effects, including reduced proliferation, migration, and EMT, alongside enhanced apoptosis.
  • Netropsin holds potential as an adjunct therapy to conventional chemotherapy for ESCC.
Keywords:
AT-rich DNA sitesHMGA proteinsepithelial–mesenchymal transitionesophageal squamous cell carcinomanetropsin

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