Targeting IRAK4 disrupts inflammatory pathways and delays tumor development in chronic lymphocytic leukemia

Leukemia. 2020 Jan;34(1):100-114. doi: 10.1038/s41375-019-0507-8. Epub 2019 Jun 13.

Abstract

Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in Toll-like receptor (TLR) signal transduction and innate immune responses. Recruitment and subsequent activation of IRAK4 upon TLR stimulation is mediated by the myeloid differentiation primary response 88 (MYD88) adaptor protein. Around 3% of chronic lymphocytic leukemia (CLL) patients have activating mutations of MYD88, a driver mutation in this disease. Here, we studied the effects of TLR activation and the pharmacological inhibition of IRAK4 with ND2158, an IRAK4 competitive inhibitor, as a therapeutic approach in CLL. Our in vitro studies demonstrated that ND2158 preferentially killed CLL cells in a dose-dependent manner. We further observed a decrease in NF-κB and STAT3 signaling, cytokine secretion, proliferation and migration of primary CLL cells from MYD88-mutated and -unmutated cases. In the Eµ-TCL1 adoptive transfer mouse model of CLL, ND2158 delayed tumor progression and modulated the activity of myeloid and T cells. Our findings show the importance of TLR signaling in CLL development and suggest IRAK4 as a therapeutic target for this disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Humans
  • Inflammation / metabolism
  • Inflammation / pathology
  • Interleukin-1 Receptor-Associated Kinases / antagonists & inhibitors
  • Interleukin-1 Receptor-Associated Kinases / pharmacology*
  • Leukemia, Lymphocytic, Chronic, B-Cell / metabolism
  • Leukemia, Lymphocytic, Chronic, B-Cell / pathology*
  • Mice
  • Mice, Inbred C57BL
  • Myeloid Differentiation Factor 88 / drug effects
  • Myeloid Differentiation Factor 88 / metabolism
  • Signal Transduction / drug effects*
  • Signal Transduction / physiology
  • Toll-Like Receptors / drug effects
  • Toll-Like Receptors / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • MYD88 protein, human
  • Myeloid Differentiation Factor 88
  • Toll-Like Receptors
  • IRAK4 protein, human
  • Interleukin-1 Receptor-Associated Kinases