Plasticity of the Mycobacterium tuberculosis respiratory chain and its impact on tuberculosis drug development

Nat Commun. 2019 Oct 31;10(1):4970. doi: 10.1038/s41467-019-12956-2.

Abstract

The viability of Mycobacterium tuberculosis (Mtb) depends on energy generated by its respiratory chain. Cytochrome bc1-aa3 oxidase and type-2 NADH dehydrogenase (NDH-2) are respiratory chain components predicted to be essential, and are currently targeted for drug development. Here we demonstrate that an Mtb cytochrome bc1-aa3 oxidase deletion mutant is viable and only partially attenuated in mice. Moreover, treatment of Mtb-infected marmosets with a cytochrome bc1-aa3 oxidase inhibitor controls disease progression and reduces lesion-associated inflammation, but most lesions become cavitary. Deletion of both NDH-2 encoding genes (Δndh-2 mutant) reveals that the essentiality of NDH-2 as shown in standard growth media is due to the presence of fatty acids. The Δndh-2 mutant is only mildly attenuated in mice and not differently susceptible to clofazimine, a drug in clinical use proposed to engage NDH-2. These results demonstrate the intrinsic plasticity of Mtb's respiratory chain, and highlight the challenges associated with targeting the pathogen's respiratory enzymes for tuberculosis drug development.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptation, Physiological / genetics
  • Animals
  • Antitubercular Agents / therapeutic use*
  • Callithrix
  • Drug Development*
  • Electron Transport
  • Electron Transport Complex III / antagonists & inhibitors
  • Electron Transport Complex III / genetics*
  • Electron Transport Complex IV / antagonists & inhibitors
  • Electron Transport Complex IV / genetics*
  • Gene Knockdown Techniques
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Lung / drug effects
  • Lung / pathology
  • Mice
  • Mycobacterium tuberculosis / drug effects
  • Mycobacterium tuberculosis / genetics*
  • Mycobacterium tuberculosis / metabolism
  • NADH Dehydrogenase / antagonists & inhibitors
  • NADH Dehydrogenase / genetics*
  • Piperidines / pharmacology
  • Pyridines / pharmacology
  • Tuberculosis / drug therapy*
  • Tuberculosis, Pulmonary / drug therapy
  • Tuberculosis, Pulmonary / pathology

Substances

  • Antitubercular Agents
  • Imidazoles
  • Piperidines
  • Pyridines
  • telacebec
  • NADH Dehydrogenase
  • Electron Transport Complex IV
  • Electron Transport Complex III