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The molecular mechanisms of 5-fluoro-2'-deoxyuridine induced cell death

A Nagano1, T Kakutani, Y Matumoto

  • 1Faculty of Pharmaceutical Sciences, Okayama University, Japan.

Insights

5-Fluoro-2'-deoxyuridine (FUdR) triggers cell death by disrupting DNA and activating endonuclease S. Protease inhibitors block this process, suggesting proteases are key downstream mediators in FUdR-induced apoptosis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cell Biology

Background:

  • 5-Fluoro-2 -deoxyuridine (FUdR) is a chemotherapeutic agent.
  • The precise molecular mechanisms underlying FUdR-induced cell death require further elucidation.

Purpose of the Study:

  • To investigate the molecular mechanism of cell death induced by 5-Fluoro-2 -deoxyuridine (FUdR).
  • To identify key enzymes and cellular events involved in FUdR-induced apoptosis.

Main Methods:

  • Investigated FUdR effects on dNTP pools and DNA integrity in mouse mammary tumor FM3A cells.
  • Isolated and characterized a novel endonuclease (endonuclease S) from FUdR-treated cells.
  • Utilized protease inhibitors to probe the role of proteases in FUdR-induced cell death.

Main Results:

  • FUdR induced dNTP pool imbalance and DNA double-strand breaks, leading to cell death.
  • A novel endonuclease S was identified, playing a crucial role in FUdR-induced DNA fragmentation.
  • Intracellular acidification preceded cell death, and endonuclease S activity in acidic conditions was implicated in DNA fragmentation.
  • Protease inhibitors blocked intracellular acidification, DNA fragmentation, and cell death, without affecting dNTP pool imbalance.

Conclusions:

  • Proteases act downstream of dNTP pool imbalance and upstream of intracellular acidification in the FUdR-induced cell death pathway.
  • Endonuclease S activation in an acidic cellular environment is a critical step in FUdR-induced DNA fragmentation and apoptosis.
  • Protease activity is essential for the progression of FUdR-induced cell death, highlighting potential therapeutic targets.

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