Arsenic trioxide inhibits the Hedgehog pathway which is aberrantly activated in acute promyelocytic leukemia

Acta Haematol. 2013;130(4):260-7. doi: 10.1159/000351603. Epub 2013 Jul 17.

Abstract

Background/aim: Dysregulated Hedgehog (Hh) signaling has been implicated in several human malignancies. Hh signaling inhibitors are predicted to have a minimal effect when the Smoothened receptor is mutated. Implications that Gli proteins are molecular targets of arsenic trioxide (ATO) action prompted us to investigate the expression of Hh signaling in acute promyelocytic leukemia (APL) and the influence of ATO on the Hh signaling pathway in APL.

Methods: Quantitative real-time reverse transcription polymerase chain reaction and Western blot were employed to analyze the expression of Hh pathway components and the influence of ATO on the Hh signaling pathway in APL.

Results: The expression of Hh pathway components was significantly upregulated in APL. In newly diagnosed APL patients, Gli2 expression was significantly positively correlated with Gli1 (R = 0.57, p < 0.001) and Smo (R = 0.56, p < 0.001) and the expression of Hh pathway components was significantly higher in the high WBC group (p < 0.05). ATO can significantly downregulate the expression of Hh pathway components in vitro and in vivo (p < 0.05).

Conclusion: The Hh pathway is aberrantly activated in APL and associated with a bad prognostic factor. ATO can effectively inhibit the expression of the Hh pathway. The obtained data give the first clinical evidence for the application of ATO in tumors exhibiting an aberrantly activated Hh pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Arsenic Trioxide
  • Arsenicals / pharmacology*
  • Arsenicals / therapeutic use
  • Cell Line, Tumor
  • Female
  • Hedgehog Proteins / antagonists & inhibitors*
  • Humans
  • Kruppel-Like Transcription Factors / biosynthesis
  • Leukemia, Promyelocytic, Acute / drug therapy
  • Leukemia, Promyelocytic, Acute / physiopathology*
  • Male
  • Middle Aged
  • Nuclear Proteins / biosynthesis
  • Oxides / pharmacology*
  • Oxides / therapeutic use
  • Patched Receptors
  • Receptors, Cell Surface / biosynthesis
  • Receptors, G-Protein-Coupled / biosynthesis
  • Smoothened Receptor
  • Transcription Factors / biosynthesis
  • Zinc Finger Protein GLI1
  • Zinc Finger Protein Gli2

Substances

  • Arsenicals
  • GLI1 protein, human
  • GLI2 protein, human
  • Hedgehog Proteins
  • Kruppel-Like Transcription Factors
  • Nuclear Proteins
  • Oxides
  • Patched Receptors
  • Receptors, Cell Surface
  • Receptors, G-Protein-Coupled
  • SMO protein, human
  • Smoothened Receptor
  • Transcription Factors
  • Zinc Finger Protein GLI1
  • Zinc Finger Protein Gli2
  • Arsenic Trioxide