[Bacterial type II topoisomerases as targets for antibacterial drugs]

Postepy Biochem. 2006;52(3):271-82.
[Article in Polish]

Abstract

Bacterial type II DNA topoisomerases are essential enzymes for correct genome functioning and cell growth. Gyrase is responsible for maintaining negative supercoiling of bacterial chromosome, whereas topoisomerase IV acts in disentangling daughter chromosomes following replication. Type II DNA topoisomerases possess an ATP binding site, which can be treated as a target for antibacterial drugs. Resolving crystal structures of protein fragments consisting of an ATP binding site complexed with ADPNP/antibiotics have proven to be valuable for the understanding of the mode of action of existing antibacterial agents and presented new possibilities for novel drug design. Coumarins, quinolones and cyclothialidines are diverse group of antibiotics that interfere with type II DNA topoisomerases, however their mode of action is different. Recently a new class of antibiotics, simociclinones, was characterized. Their mechanism of action towards gyrase is entirely distinct from already known modes of action, therefore demonstrating the potential for development of novel anti-bacterial agents.

Publication types

  • English Abstract
  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects*
  • Bacteria / enzymology*
  • Binding Sites
  • DNA Topoisomerases, Type II / drug effects*
  • DNA Topoisomerases, Type II / metabolism*
  • Drug Resistance, Bacterial
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Models, Molecular
  • Topoisomerase II Inhibitors

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Topoisomerase II Inhibitors
  • DNA Topoisomerases, Type II