LspA-independent action of globomycin on Mycobacterium tuberculosis

J Antimicrob Chemother. 2007 Aug;60(2):414-6. doi: 10.1093/jac/dkm223. Epub 2007 Jun 19.

Abstract

Objectives: The objective of this study was to investigate the antimicrobial activity and specificity of globomycin, an inhibitor of lipoprotein signal peptidase II (LspA), against Mycobacterium tuberculosis.

Methods: The mycobactericidal and mycobacteriostatic activity of globomycin was determined by optical density and cfu plating. The specificity of globomycin was determined by western immunoblotting using anti-MPT83 antibody.

Results: Globomycin is mycobactericidal at concentrations>or=40 mg/L. However, at 80 mg/L, the processing of the lipoprotein MPT-83 is unaffected and growth-inhibitory effect of globomycin is unchanged in an lspA null mutant (DeltalspA::lspAmut) lacking the putative drug target.

Conclusions: Globomycin kills M. tuberculosis through a mechanism that is independent of LspA.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Aspartic Acid Endopeptidases / antagonists & inhibitors*
  • Aspartic Acid Endopeptidases / physiology*
  • Bacterial Proteins / antagonists & inhibitors*
  • Bacterial Proteins / physiology*
  • Blotting, Western
  • Dose-Response Relationship, Drug
  • Kinetics
  • Mutation
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / growth & development
  • Mycobacterium tuberculosis / physiology
  • Peptides / pharmacology*
  • Protease Inhibitors / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Peptides
  • Protease Inhibitors
  • globomycin
  • Aspartic Acid Endopeptidases
  • signal peptidase II