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Cyclosporine inhibition of angiogenesis involves the transcription factor HESR1

Gaurang Shah1, Frank A Middleton, Karen L Gentile

  • 1Department of Surgery, SUNY Upstate Medical University, Syracuse, New York 13210, USA.

The Journal of Surgical Research
|August 13, 2008
PubMed
Abstract

Insights

Cyclosporine A (CyA) inhibits angiogenesis by increasing HESR1 expression and decreasing VEGFR2. This suggests high-dose CyA may treat diseases dependent on blood vessel growth.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Immunology

Background:

  • Angiogenesis is crucial for development and tumor growth.
  • Cyclosporine A (CyA) experimentally inhibits angiogenesis.
  • Mechanisms of CyA's antiangiogenic effects require further elucidation.

Purpose of the Study:

  • Investigate nuclear factors involved in CyA's antiangiogenic effects.
  • Analyze gene expression changes in human aortic endothelial cells (HAEC) treated with CyA and FK 506.
  • Identify specific molecular pathways targeted by CyA.

Main Methods:

  • HAEC were treated with varying doses of CyA (2 and 10 microg/mL) or FK 506 (1 microg/mL).
  • Gene expression profiling was performed using Affymetrix GeneChip U133-A.
  • Quantitative reverse transcription-polymerase chain reaction (RT-PCR) validated key findings.

Main Results:

  • CyA treatment significantly increased hairy enhancer of split-related protein 1 (HESR1) expression (44- to 57-fold).
  • CyA treatment down-regulated vascular endothelial growth factor receptor 2 (VEGFR2) transcripts (1.73- to 1.93-fold).
  • FK 506 did not affect HESR1 expression, indicating a CyA-specific effect.

Conclusions:

  • CyA exhibits antiangiogenic properties.
  • Overexpression of HESR1 and down-regulation of VEGFR2 are key mechanisms.
  • High-dose CyA presents a potential novel therapeutic strategy for angiogenesis-dependent diseases.

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