Recent developments in topoisomerase-targeted cancer chemotherapy

KirkE Hevener1, Tatsiana A Verstak1, Katie E Lutat1

  • 1Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, USA.

Insights

DNA topoisomerase enzymes are crucial for cell function and are targeted by cancer drugs. This review covers current and developing topoisomerase inhibitors for cancer treatment.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • DNA topoisomerases are vital enzymes regulating DNA topology during replication and transcription.
  • These enzymes are key targets for antimicrobial and anticancer chemotherapeutic agents.
  • Natural products like camptothecin and anthracyclines are established cancer treatments.

Purpose of the Study:

  • To review clinically used topoisomerase inhibitors for cancer therapy.
  • To discuss the pharmacology and chemistry of novel topoisomerase inhibitors in development.

Main Methods:

  • Literature review of existing and emerging topoisomerase inhibitors.
  • Analysis of clinical and preclinical data on drug efficacy and mechanisms.

Main Results:

  • Overview of established topoisomerase inhibitors in cancer treatment.
  • Identification of promising new agents in clinical and preclinical stages.

Conclusions:

  • Targeting DNA topoisomerases remains a critical strategy in cancer therapy.
  • Ongoing research focuses on developing more selective and effective inhibitors.

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