PARP inhibition selectively increases sensitivity to cisplatin in ERCC1-low non-small cell lung cancer cells

Carcinogenesis. 2013 Apr;34(4):739-49. doi: 10.1093/carcin/bgs393. Epub 2012 Dec 28.

Abstract

Platinum compounds are the foundation of chemotherapy regimens for non-small cell lung cancer (NSCLC) despite poor response rates and limited response duration. It has been reported that tumor expression of excision repair cross-complementation group 1 (ERCC1), a key component in nucleotide excision repair, may correlate with clinical response to platinum agents. We found that most primary lung tumor specimens demonstrated a stronger protein expression of poly (adenosine diphosphate ribose) polymerases 1 (PARP1) than their normal counterparts. Therefore, we hypothesized that combining PARP inhibition with platinum compounds may be an approach to improve platinum-based therapy for NSCLC. Drug combination experiments revealed that two distinct PARP inhibitors, olaparib and veliparib, not only potentiated the cell killing by cisplatin but also conferred cytotoxicity as a single agent specifically in ERCC1-low HCC827 and PC9 but not in ERCC1-high A549 and H157 lung cancer cells. Moreover, small interfering RNA knockdown of ERCC1 in A549 and H157 cells increased their sensitivities to both cisplatin and olaparib in a synergistic manner in our model. Furthermore, mechanistic studies indicated that combined PARP inhibitor and cisplatin could lead to sustained DNA double-strand breaks, prolonged G2/M cell cycle arrest with distinct activation of checkpoint kinase 1 signaling and more pronounced apoptosis preferentially in lung cancer cells with low ERCC1 expression. Collectively, these data suggest that there is a synergistic relationship between PARP inhibition and low ERCC1 expression in NSCLC that could be exploited for novel therapeutic approaches in lung cancer therapy based on tumor ERCC1 expression.

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols
  • Apoptosis / drug effects
  • Benzimidazoles / pharmacology
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Non-Small-Cell Lung / metabolism
  • Cell Line, Tumor
  • Checkpoint Kinase 1
  • Cisplatin / pharmacology*
  • DNA Breaks, Double-Stranded / drug effects
  • DNA-Binding Proteins / biosynthesis*
  • DNA-Binding Proteins / genetics
  • Drug Synergism
  • Endonucleases / biosynthesis*
  • Endonucleases / genetics
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / genetics
  • Lung Neoplasms / metabolism
  • Phthalazines / pharmacology
  • Piperazines / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Poly(ADP-ribose) Polymerases / biosynthesis
  • Protein Kinases / metabolism
  • RNA Interference
  • RNA, Small Interfering

Substances

  • Antineoplastic Agents
  • Benzimidazoles
  • DNA-Binding Proteins
  • Phthalazines
  • Piperazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • RNA, Small Interfering
  • veliparib
  • Poly(ADP-ribose) Polymerases
  • Protein Kinases
  • CHEK1 protein, human
  • Checkpoint Kinase 1
  • ERCC1 protein, human
  • Endonucleases
  • Cisplatin
  • olaparib