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Protein arginine deiminase 4: A target for an epigenetic cancer therapy

Academic Article
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Overview

authors

  • Slack, J. L.
  • Causey, C. P.
  • Thompson, Paul

publication date

  • February 2011

journal

  • Cellular and Molecular Life Sciences  Journal

abstract

  • The recent approvals of anticancer therapeutic agents targeting the histone deacetylases and DNA methyltransferases have highlighted the important role that epigenetics plays in human diseases, and suggested that the factors controlling gene expression are novel drug targets. Protein arginine deiminase 4 (PAD4) is one such target because its effects on gene expression parallel those observed for the histone deacetylases. We demonstrated that F- and Cl-amidine, two potent PAD4 inhibitors, display micromolar cytotoxic effects towards several cancerous cell lines (HL-60, MCF7 and HT-29); no effect was observed in noncancerous lines (NIH 3T3 and HL-60 granulocytes). These compounds also induced the differentiation of HL-60 and HT29 cells. Finally, these compounds synergistically potentiated the cell killing effects of doxorubicin. Taken together, these findings suggest PAD4 inhibition as a novel epigenetic approach for the treatment of cancer, and suggest that F- and Cl-amidine are candidate therapeutic agents for this disease.

subject areas

  • Amidines
  • Animals
  • Antibiotics, Antineoplastic
  • Antigens, CD38
  • Antineoplastic Agents
  • Cell Differentiation
  • Cell Line, Tumor
  • Cell Survival
  • Cyclin-Dependent Kinase Inhibitor p21
  • Doxorubicin
  • Drug Synergism
  • Enzyme Inhibitors
  • Epigenomics
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Hydrolases
  • Neoplasms
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Research

keywords

  • Citrulline
  • Epigenetics
  • HL-60
  • Haloacetamidine
  • Inhibition
  • Protein arginine deiminase
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Identity

PubMed Central ID

  • PMC3815436

International Standard Serial Number (ISSN)

  • 1420-682X

Digital Object Identifier (DOI)

  • 10.1007/s00018-010-0480-x

PubMed ID

  • 20706768
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Additional Document Info

start page

  • 709

end page

  • 720

volume

  • 68

issue

  • 4

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