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Telomere inhibition and telomere disruption as processes for drug targeting

Evonne M Rezler1, David J Bearss, Laurence H Hurley

  • 1College of Pharmacy, The University of Arizona, Tucson, Arizona 85721, USA. rezler@pharmacy.arizona.edu

Annual Review of Pharmacology and Toxicology
|January 24, 2003
PubMed

Insights

Anticancer strategies targeting telomerase and telomeres show promise. Inhibitors like antisense oligonucleotides, ribozymes, and G-quadruplex stabilizers offer new therapeutic avenues for cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Telomerase and telomeric DNA are key targets for anticancer drugs.
  • Telomere dysfunction is linked to cancer development and progression.

Purpose of the Study:

  • To review recent advances in telomerase inhibition strategies.
  • To focus on telomeres, telomerase, and their roles in anticancer agent design.

Main Methods:

  • Review of antisense oligonucleotides and ribozymes targeting telomerase mRNA and hTR RNA.
  • Analysis of drugs binding to telomeres and stabilizing G-quadruplex structures.

Main Results:

  • Antisense oligonucleotides and ribozymes are potent catalytic inhibitors but have delayed clinical effectiveness.
  • Telomere-binding drugs stabilizing G-quadruplexes are also effective telomerase inhibitors.

Conclusions:

  • Telomere-targeting agents, including G-quadruplex stabilizers, represent a promising approach for cancer therapy.
  • Understanding telomere biology is crucial for designing effective anticancer drugs targeting telomerase.

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