Targeting telomeres and telomerase

Anne De Cian1, Laurent Lacroix, Céline Douarre

  • 1INSERM, U565, Acides nucléiques: dynamique, ciblage et fonctions biologiques, 43 rue Cuvier, CP26, Paris Cedex 05, F-75231, France.

Biochimie
|September 8, 2007
PubMed

Insights

Telomeres and telomerase are promising cancer therapy targets. This review focuses on G-quadruplex ligands as telomerase inhibitors and their potential in oncology.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Telomeres protect chromosome ends, and their maintenance by telomerase is crucial for cancer cell proliferation.
  • Telomerase activity is dysregulated in most human cancers, making it a prime target for therapeutic intervention.
  • Understanding telomere biology and telomerase function is key to developing novel anti-cancer strategies.

Purpose of the Study:

  • To review the latest mechanisms of action for telomerase inhibitors.
  • To highlight G-quadruplex ligands as a specific class of telomere-targeting agents.
  • To discuss the potential clinical applications of these inhibitors in cancer treatment.

Main Methods:

  • Literature review of preclinical and clinical studies on telomerase inhibitors.
  • Focus on G-quadruplex ligands and their interaction with telomeric DNA.
  • Analysis of data regarding the efficacy and safety of these agents in cancer models.

Main Results:

  • Telomerase inhibitors, particularly G-quadruplex ligands, demonstrate potent anti-cancer activity by disrupting telomere maintenance.
  • These ligands stabilize G-quadruplex structures in telomeric DNA, inhibiting telomerase function.
  • Evidence suggests a strong correlation between G-quadruplex ligand efficacy and telomere length/telomerase activity in cancer cells.

Conclusions:

  • G-quadruplex ligands represent a promising class of telomerase inhibitors for cancer therapy.
  • Targeting telomeres and telomerase offers a viable strategy to combat cancer.
  • Further research and clinical trials are warranted to fully explore the therapeutic potential of G-quadruplex ligands in oncology.

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