Combined chemical genetics and data-driven bioinformatics approach identifies receptor tyrosine kinase inhibitors as host-directed antimicrobials

Nat Commun. 2018 Jan 24;9(1):358. doi: 10.1038/s41467-017-02777-6.

Abstract

Antibiotic resistance poses rapidly increasing global problems in combatting multidrug-resistant (MDR) infectious diseases like MDR tuberculosis, prompting for novel approaches including host-directed therapies (HDT). Intracellular pathogens like Salmonellae and Mycobacterium tuberculosis (Mtb) exploit host pathways to survive. Only very few HDT compounds targeting host pathways are currently known. In a library of pharmacologically active compounds (LOPAC)-based drug-repurposing screen, we identify multiple compounds, which target receptor tyrosine kinases (RTKs) and inhibit intracellular Mtb and Salmonellae more potently than currently known HDT compounds. By developing a data-driven in silico model based on confirmed targets from public databases, we successfully predict additional efficacious HDT compounds. These compounds target host RTK signaling and inhibit intracellular (MDR) Mtb. A complementary human kinome siRNA screen independently confirms the role of RTK signaling and kinases (BLK, ABL1, and NTRK1) in host control of Mtb. These approaches validate RTK signaling as a drugable host pathway for HDT against intracellular bacteria.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Cell Line
  • Computational Biology
  • Drug Resistance, Bacterial
  • Enzyme Inhibitors / pharmacology*
  • Host-Pathogen Interactions / drug effects
  • Humans
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / genetics
  • Mycobacterium tuberculosis / physiology
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Receptor Protein-Tyrosine Kinases / genetics
  • Receptor Protein-Tyrosine Kinases / metabolism
  • Salmonella Infections / enzymology*
  • Salmonella Infections / genetics
  • Salmonella Infections / microbiology
  • Salmonella typhimurium / drug effects*
  • Salmonella typhimurium / genetics
  • Salmonella typhimurium / physiology
  • Signal Transduction / drug effects
  • Tuberculosis / enzymology*
  • Tuberculosis / genetics
  • Tuberculosis / microbiology

Substances

  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Receptor Protein-Tyrosine Kinases