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Cangrelor alleviates pulmonary fibrosis by inhibiting GPR17-mediated inflammation in mice

Tian-Wei Zhan1, Yu-Xin Tian2, Qi Wang1

  • 1Department of Thoracic Surgery, The Second Affiliated Hospital of Zhejiang University School of Medicine, 88 Jie-Fang Road, Hangzhou, Zhejiang 310009, China.

International Immunopharmacology
|July 24, 2018
PubMed

Insights

Cangrelor, an anti-platelet drug, reduces inflammation and fibrosis in the lungs. This study shows cangrelor suppresses G protein-coupled receptor 17 (GPR17)-mediated inflammation, offering potential for treating pulmonary fibrosis.

Area of Science:

  • Pulmonary Medicine
  • Immunology
  • Pharmacology

Background:

  • Pulmonary fibrosis is a severe lung condition where macrophages drive disease progression.
  • G protein-coupled receptor 17 (GPR17) is implicated in inflammatory processes, including allergic pulmonary inflammation.
  • Cangrelor, an anti-platelet agent, acts as a non-selective GPR17 antagonist.

Purpose of the Study:

  • To investigate the therapeutic potential of cangrelor in bleomycin (BLM)-induced pulmonary fibrosis.
  • To examine the role of GPR17 in BLM-induced macrophage inflammation and lung fibrosis.
  • To determine if cangrelor mitigates pulmonary fibrosis by inhibiting GPR17-mediated inflammation.

Main Methods:

  • Assessed the effects of cangrelor on BLM-induced RAW 264.7 macrophage inflammation.
  • Evaluated GPR17 expression and inflammatory cytokine production (TNF-α, IL-6, TGF-β1) in macrophages.
  • Administered cangrelor to C57BL/6J mice with BLM-induced pulmonary fibrosis and analyzed lung tissue.

Main Results:

  • BLM increased GPR17 expression and inflammatory cytokine release in macrophages.
  • GPR17 knockdown attenuated BLM-induced inflammatory responses.
  • Cangrelor significantly reduced macrophage inflammation and pulmonary fibrosis in a dose-dependent manner, decreasing GPR17-positive macrophages and cytokine levels.

Conclusions:

  • Cangrelor alleviates bleomycin-induced pulmonary fibrosis by suppressing GPR17-mediated inflammation.
  • GPR17 plays a key role in macrophage-driven inflammation and fibrosis development.
  • Cangrelor demonstrates potential as a novel therapeutic agent for pulmonary fibrosis.
Keywords:
CangrelorGPR17Inflammatory cytokinesMacrophagesPulmonary fibrosis

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