DNA topoisomerases as targets for anticancer drugs

J Clin Pharm Ther. 2001 Dec;26(6):405-16. doi: 10.1046/j.1365-2710.2001.00368.x.


DNA topoisomerases are essential enzymes that regulate the conformational changes in DNA topology by catalysing the concerted breakage and rejoining of DNA strands during normal cellular growth. Over the past few years there has been considerable pharmacological interest in these enzymes because inhibitors of DNA topoisomerases represent a major class of anticancer drugs. This review highlights topoisomerase-targeting drugs that have shown promising anticancer activities. The mechanisms by which those drugs interfere with the catalytic cycles of type I and type II DNA topoisomerases and the factors involved in the development of resistance to these drugs are discussed.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Catalysis
  • DNA Damage
  • DNA Repair
  • DNA Topoisomerases, Type I / drug effects*
  • DNA Topoisomerases, Type I / metabolism*
  • DNA Topoisomerases, Type II / drug effects*
  • DNA Topoisomerases, Type II / metabolism*
  • Drug Resistance, Multiple
  • Drug Resistance, Neoplasm
  • Humans


  • Antineoplastic Agents
  • DNA Topoisomerases, Type I
  • DNA Topoisomerases, Type II