Efflux pumps: their role in antibacterial drug discovery

Curr Med Chem. 2001 Dec;8(14):1699-711. doi: 10.2174/0929867013371743.


The emergence of active efflux as a major causative factor in antibiotic resistance has been one of the most significant trends in antiinfective chemotherapy over the last decade. The phenomenon affects virtually all classes of antibiotics and frequently results in multi-drug resistant phenotypes. This review analyzes efflux pumps of clinical significance and examines their impact on different antibiotic classes relative to other mechanisms of resistance. Progress in strategies to combat efflux-mediated resistance by modification of existing antibiotics or identification of efflux pump inhibitors is also reviewed.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Antiporters / antagonists & inhibitors
  • Bacterial Proteins / antagonists & inhibitors
  • Bacterial Proteins / chemistry
  • Bacterial Proteins / drug effects
  • Bacterial Proteins / physiology*
  • Dipeptides / chemistry
  • Dipeptides / pharmacology
  • Drug Design*
  • Drug Resistance, Multiple, Bacterial / physiology*
  • Humans
  • Multidrug Resistance-Associated Proteins


  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antiporters
  • Bacterial Proteins
  • Dipeptides
  • Multidrug Resistance-Associated Proteins
  • phenylalanine arginine beta-naphthylamide
  • tetA protein, Bacteria
  • NorA protein, Staphylococcus