Interleukin-1 receptor-associated kinase 4 (IRAK4) is a critical regulator of inflammatory signalling through toll-like receptors 4 and 7/8 in murine and human lungs

Br J Pharmacol. 2024 Nov;181(22):4647-4657. doi: 10.1111/bph.16509. Epub 2024 Aug 13.

Abstract

Background and purpose: Toll-like receptors 4 (TLR4) and TLR7/TLR8 play an important role in mediating the inflammatory effects of bacterial and viral pathogens. Interleukin-1 receptor-associated kinase 4 (IRAK4) is an important regulator of signalling by toll-like receptor (TLR) and hence is a potential therapeutic target in diseases characterized by increased lung inflammatory signalling.

Experimental approach: We used an established murine model of acute lung inflammation, and studied human lung tissue ex vivo, to investigate the effects of inhibiting IRAK4 on lung inflammatory pathways.

Key results: We show that TLR4 stimulation produces an inflammatory response characterized by neutrophil influx and tumour necrosis factor-α (TNF-α) production in murine lungs and that these responses are markedly reduced in IRAK4 kinase-dead mice. In addition, we characterize a novel selective IRAK4 inhibitor, BI1543673, and show that this compound can reduce lipopolysaccharide (LPS)-induced airway inflammation in wild-type mice. Additionally, BI1543673 reduced inflammatory responses to both TLR4 and TLR7/8 stimulation in human lung tissue studied ex vivo.

Conclusion and implications: These data demonstrate a key role for IRAK4 signalling in lung inflammation and suggest that IRAK4 inhibition has potential utility to treat lung diseases characterized by inflammatory responses driven through TLR4 and TLR7/8.

Keywords: IRAK4; chronic obstructive pulmonary disease; exacerbations; interstitial lung disease; lung inflammation; toll‐ like receptors.

MeSH terms

  • Animals
  • Humans
  • Interleukin-1 Receptor-Associated Kinases* / antagonists & inhibitors
  • Interleukin-1 Receptor-Associated Kinases* / metabolism
  • Lipopolysaccharides / pharmacology
  • Lung* / drug effects
  • Lung* / immunology
  • Lung* / metabolism
  • Male
  • Membrane Glycoproteins / antagonists & inhibitors
  • Membrane Glycoproteins / metabolism
  • Mice
  • Mice, Inbred C57BL*
  • Mice, Knockout
  • Pneumonia / immunology
  • Pneumonia / metabolism
  • Signal Transduction* / drug effects
  • Toll-Like Receptor 4* / antagonists & inhibitors
  • Toll-Like Receptor 4* / metabolism
  • Toll-Like Receptor 7* / metabolism
  • Toll-Like Receptor 8* / antagonists & inhibitors
  • Toll-Like Receptor 8* / metabolism
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Interleukin-1 Receptor-Associated Kinases
  • Toll-Like Receptor 4
  • IRAK4 protein, human
  • Toll-Like Receptor 7
  • Toll-Like Receptor 8
  • Irak4 protein, mouse
  • Tumor Necrosis Factor-alpha
  • Tlr7 protein, mouse
  • Lipopolysaccharides
  • TLR8 protein, human
  • TLR8 protein, mouse
  • Membrane Glycoproteins
  • Tlr4 protein, mouse