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DNA topoisomerase I and DNA gyrase as targets for TB therapy

Valakunja Nagaraja1, Adwait A Godbole2, Sara R Henderson3

  • 1Department of Microbiology and Cell Biology, Indian Institute of Science, Bangalore 560 012, India; Jawaharlal Nehru Centre for Advanced Scientific Research, Bangalore 560064, India.

Drug Discovery Today
|November 19, 2016
PubMed

Insights

New drugs targeting DNA topoisomerases are crucial for combating tuberculosis (TB), a deadly bacterial disease. This review explores targeting DNA topoisomerase I and DNA gyrase in Mycobacterium tuberculosis.

Area of Science:

  • Microbiology
  • Molecular Biology
  • Drug Discovery

Background:

  • Tuberculosis (TB) remains a leading cause of bacterial death globally.
  • Antimicrobial resistance necessitates novel therapeutic agents.
  • DNA topoisomerases are validated targets for antimicrobial therapies.

Purpose of the Study:

  • To review the use of topoisomerases as antibacterial targets.
  • To summarize progress in developing new agents against Mycobacterium tuberculosis topoisomerases.

Main Methods:

  • Literature review of topoisomerase as antibacterial targets.
  • Summary of research on agents targeting DNA gyrase and topoisomerase I in M. tuberculosis.

Main Results:

  • DNA gyrase is a well-established target, with fluoroquinolones being clinically successful.
  • DNA topoisomerase I from M. tuberculosis is an underexplored but promising target.
  • Progress is being made in developing novel agents for both targets.

Conclusions:

  • Targeting DNA topoisomerases offers a viable strategy for new TB therapies.
  • Further research into DNA topoisomerase I inhibitors is warranted.
  • Developing new agents against M. tuberculosis topoisomerases is critical for overcoming drug resistance.

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