A PCNA-derived cell permeable peptide selectively inhibits neuroblastoma cell growth

PLoS One. 2014 Apr 11;9(4):e94773. doi: 10.1371/journal.pone.0094773. eCollection 2014.

Abstract

Proliferating cell nuclear antigen (PCNA), through its interaction with various proteins involved in DNA synthesis, cell cycle regulation, and DNA repair, plays a central role in maintaining genome stability. We previously reported a novel cancer associated PCNA isoform (dubbed caPCNA), which was significantly expressed in a broad range of cancer cells and tumor tissues, but not in non-malignant cells. We found that the caPCNA-specific antigenic site lies between L126 and Y133, a region within the interconnector domain of PCNA that is known to be a major binding site for many of PCNA's interacting proteins. We hypothesized that therapeutic agents targeting protein-protein interactions mediated through this region may confer differential toxicity to normal and malignant cells. To test this hypothesis, we designed a cell permeable peptide containing the PCNA L126-Y133 sequence. Here, we report that this peptide selectively kills human neuroblastoma cells, especially those with MYCN gene amplification, with much less toxicity to non-malignant human cells. Mechanistically, the peptide is able to block PCNA interactions in cancer cells. It interferes with DNA synthesis and homologous recombination-mediated double-stranded DNA break repair, resulting in S-phase arrest, accumulation of DNA damage, and enhanced sensitivity to cisplatin. These results demonstrate conceptually the utility of this peptide for treating neuroblastomas, particularly, the unfavorable MYCN-amplified tumors.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Membrane Permeability*
  • Cell Proliferation / drug effects
  • DNA Breaks, Double-Stranded / drug effects
  • DNA Replication / drug effects
  • Disease Models, Animal
  • Drug Resistance, Neoplasm
  • Humans
  • Neuroblastoma / metabolism*
  • Neuroblastoma / pathology
  • Peptide Fragments / metabolism*
  • Peptide Fragments / pharmacology*
  • Proliferating Cell Nuclear Antigen / chemistry
  • Proliferating Cell Nuclear Antigen / metabolism*
  • Protein Binding / drug effects
  • S Phase Cell Cycle Checkpoints / drug effects
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Peptide Fragments
  • Proliferating Cell Nuclear Antigen