The histamine analogue clobenpropit modulates IRF7 phosphorylation and interferon production by targeting CXCR4 in systemic lupus erythematosus models

Front Immunol. 2024 Dec 16:15:1490593. doi: 10.3389/fimmu.2024.1490593. eCollection 2024.

Abstract

Introduction: Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by an overactive immune response, particularly involving excessive production of type I interferons. This overproduction is driven by the phosphorylation of IRF7, a crucial factor in interferon gene activation. Current treatments for SLE are often not very effective and can have serious side effects.

Methods: Our study introduces clobenpropit, a histamine analogue, as a potential new therapy targeting the CXCR4 receptor to reduce IRF7 phosphorylation and subsequent interferon production. We employed various laboratory techniques to investigate how clobenpropit interacts with CXCR4 and its effects on immune cells from healthy individuals and SLE patients.

Results: Clobenpropit binds effectively to CXCR4, significantly inhibiting IRF7 phosphorylation and reducing interferon production. Additionally, clobenpropit lowered levels of pro-inflammatory cytokines in a mouse model of lupus, demonstrating efficacy comparable to the standard treatment, prednisolone.

Discussion: These results suggest that clobenpropit could be a promising new treatment for SLE, offering a targeted approach with potential advantages over current therapies.

Keywords: CXCR4; SLE; interferons; pDc; pIRF7.

MeSH terms

  • Animals
  • Disease Models, Animal*
  • Female
  • Histamine / metabolism
  • Humans
  • Imidazoles / pharmacology
  • Interferon Regulatory Factor-7* / metabolism
  • Interferons / metabolism
  • Lupus Erythematosus, Systemic* / drug therapy
  • Lupus Erythematosus, Systemic* / immunology
  • Lupus Erythematosus, Systemic* / metabolism
  • Mice
  • Phosphorylation
  • Receptors, CXCR4* / metabolism

Substances

  • Receptors, CXCR4
  • Interferon Regulatory Factor-7
  • CXCR4 protein, human
  • Histamine
  • IRF7 protein, human
  • Interferons
  • Imidazoles

Grants and funding

The author(s) declare financial support was received for the research, authorship, and/or publication of this article. This work was supported by a European Union’s Horizon Europe MSCA Individual Fellowship under grant agreement 101063953 (SMiPAX4), a grant by the French national research agency ANR-21-CE15-0048 (InflamX4) and ANRS-MIE (SF/SA/n°1038).