Potentiation of antibacterial activity of the MB-1 siderophore-monobactam conjugate using an efflux pump inhibitor

Antimicrob Agents Chemother. 2015 Apr;59(4):2439-42. doi: 10.1128/AAC.04172-14. Epub 2015 Jan 20.

Abstract

Preliminary enthusiasm over the encouraging spectrum and in vitro activities of siderophore conjugates, such as MB-1, was recently tempered by unexpected variability in in vivo efficacy. The need for these conjugates to compete for iron with endogenously produced siderophores has exposed a significant liability for this novel antibacterial strategy. Here, we have exploited dependence on efflux for siderophore secretion in Pseudomonas aeruginosa and provide evidence that efflux inhibition may circumvent this in vivo-relevant resistance liability.

MeSH terms

  • ATP-Binding Cassette Transporters / antagonists & inhibitors
  • Anti-Bacterial Agents / pharmacology*
  • Drug Resistance, Bacterial / drug effects
  • Drug Resistance, Bacterial / genetics
  • Microbial Sensitivity Tests
  • Monobactams / pharmacology*
  • Mutation
  • Pseudomonas aeruginosa / drug effects
  • Pseudomonas aeruginosa / enzymology
  • Pyridones / pharmacology*
  • Reserpine / pharmacology
  • Siderophores / pharmacology*

Substances

  • ATP-Binding Cassette Transporters
  • Anti-Bacterial Agents
  • MB-1 monobactam compound
  • Monobactams
  • Pyridones
  • Siderophores
  • Reserpine