MmpL3 Inhibition: A New Approach to Treat Nontuberculous Mycobacterial Infections

Int J Mol Sci. 2020 Aug 27;21(17):6202. doi: 10.3390/ijms21176202.

Abstract

Outside of Mycobacterium tuberculosis and Mycobacterium leprae, nontuberculous mycobacteria (NTM) are environmental mycobacteria (>190 species) and are classified as slow- or rapid-growing mycobacteria. Infections caused by NTM show an increased incidence in immunocompromised patients and patients with underlying structural lung disease. The true global prevalence of NTM infections remains unknown because many countries do not require mandatory reporting of the infection. This is coupled with a challenging diagnosis and identification of the species. Current therapies for treatment of NTM infections require multidrug regimens for a minimum of 18 months and are associated with serious adverse reactions, infection relapse, and high reinfection rates, necessitating discovery of novel antimycobacterial agents. Robust drug discovery processes have discovered inhibitors targeting mycobacterial membrane protein large 3 (MmpL3), a protein responsible for translocating mycolic acids from the inner membrane to periplasm in the biosynthesis of the mycobacterial cell membrane. This review focuses on promising new chemical scaffolds that inhibit MmpL3 function and represent interesting and promising putative drug candidates for the treatment of NTM infections. Additionally, agents (FS-1, SMARt-420, C10) that promote reversion of drug resistance are also reviewed.

Keywords: MmpL3; Mycobacterium abscessus; mycolic acid; nontuberculous mycobacteria; susceptibility reversion.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Bacterial Proteins / metabolism
  • Biological Transport / drug effects
  • Drug Discovery
  • Drug Resistance, Multiple, Bacterial / drug effects
  • Gene Expression Regulation, Bacterial / drug effects
  • Humans
  • Iodophors / pharmacology
  • Iodophors / therapeutic use
  • Isoxazoles / pharmacology
  • Isoxazoles / therapeutic use
  • Membrane Transport Proteins / metabolism*
  • Mycobacterium Infections, Nontuberculous / drug therapy*
  • Mycobacterium Infections, Nontuberculous / metabolism
  • Mycolic Acids / metabolism
  • Nontuberculous Mycobacteria / drug effects
  • Nontuberculous Mycobacteria / metabolism*
  • Polysaccharides / pharmacology
  • Polysaccharides / therapeutic use
  • Spiro Compounds / pharmacology
  • Spiro Compounds / therapeutic use

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Iodophors
  • Isoxazoles
  • Membrane Transport Proteins
  • Mycolic Acids
  • Polysaccharides
  • SMARt-420
  • Spiro Compounds
  • pharmaceutical FS-1