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Modulation of CXCR4 expression and SDF-1alpha functional activity during differentiation of human monocytes and

S K Gupta1, K Pillarisetti, P G Lysko

  • 1Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA. Shalley_K_Gupta@sbphrd.com

Insights

Monocyte chemoattraction via stromal cell-derived factor-1alpha (SDF-1alpha) and CXCR4 is key in vascular diseases. Oxidized LDL induces CXCR4 re-expression in foam cells, suggesting a role in atherosclerosis progression.

Area of Science:

  • Immunology
  • Vascular Biology
  • Molecular Biology

Background:

  • The CXC chemokine stromal cell-derived factor-1alpha (SDF-1alpha) and its receptor CXCR4 mediate monocyte chemoattraction, potentially contributing to vascular diseases like atherosclerosis.
  • Understanding the regulation of CXCR4 in monocytes during differentiation is crucial for elucidating its role in disease pathogenesis.

Purpose of the Study:

  • To investigate the regulation of CXCR4 transcription and SDF-1-induced functional responses in human monocytes during differentiation.
  • To examine the effects of granulocyte-macrophage colony-stimulating factor (GM-CSF), oxidized low-density lipoprotein (Ox-LDL), and unmodified LDL on CXCR4 expression and function.

Main Methods:

  • Studied human monocyte differentiation in the presence of GM-CSF, Ox-LDL, and LDL.
  • Utilized HL-60 cells induced with phorbol myristate acetate (PMA) to model CXCR4 expression dynamics.
  • Assessed CXCR4 mRNA levels and SDF-1-mediated calcium influx ([Ca2+]i).
  • Employed flow cytometry to analyze surface CXCR4 expression.

Main Results:

  • SDF-1-mediated calcium influx in monocytes initially declines post-isolation but gradually recovers with concomitant re-expression of CXCR4 mRNA.
  • Oxidized LDL significantly induces CXCR4 mRNA (3-4 fold) in macrophage-derived foam cells.
  • PMA-induced HL-60 cells show rapid CXCR4 mRNA stimulation followed by decline and eventual restoration, mirroring monocyte patterns.
  • Surface CXCR4 expression is maintained on PMA-treated HL-60 cells; GM-CSF does not affect CXCR4 mRNA in HL-60 cells or human macrophages.

Conclusions:

  • CXCR4 expression and function in monocytes are dynamically regulated during differentiation and influenced by factors like Ox-LDL.
  • Oxidized LDL-induced CXCR4 re-expression in foam cells may promote their involvement in atherosclerotic plaque development.
  • The findings provide insights into the molecular mechanisms underlying monocyte behavior in vascular disease contexts.

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