The Correlation Between PARP1 and BRCA1 in AR Positive Triple-negative Breast Cancer

Int J Biol Sci. 2016 Nov 25;12(12):1500-1510. doi: 10.7150/ijbs.16176. eCollection 2016.

Abstract

Triple-negative breast cancer (TNBC) lacks estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER-2) expression and thus cannot benefit from conventional hormonal or anti-HER2 targeted therapies. Anti-androgen therapy has shown a certain effect on androgen receptor (AR) positive TNBC. The emerging researches have proved that poly (ADP-ribose) polymerase (PARP) inhibitor is effective in BRCA1-deficient breast cancers. We demonstrated that combination of AR antagonist (bicalutamide) and PARP inhibitor (ABT-888) could inhibit cell viability and induce cell apoptosis significantly whatever in vitro or in vivo setting in AR-positive TNBC. Previous studies have proved that both BRCA1 and PARP1 have close connections with AR in prostate cancer. We explored the correlation among AR, PARP1 and BRCA1 in TNBC for the first time. After BRCA1 overexpression, the expression of AR and PARP1 were decreased in mRNA and protein levels. Additionally, AR positively regulated PARP1 while PARP1 also up-regulated AR expression in vitro. We also confirmed BRCA1 expression was negatively correlated with AR and PARP1 in TNBC patients using a tissue microarray with TNBC patient samples. These results suggest that the combination of bicalutamide and PARP inhibitor may be a potential strategy for TNBC patients and merits further evaluation.

Keywords: AR; BRCA1; PARP1; combination therapy; triple-negative breast cancer..

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anilides / therapeutic use
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Apoptosis / drug effects
  • BRCA1 Protein / genetics
  • BRCA1 Protein / metabolism*
  • Benzimidazoles / therapeutic use
  • Blotting, Western
  • Cell Line
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Female
  • Flow Cytometry
  • Humans
  • Immunohistochemistry
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nitriles / therapeutic use
  • Poly (ADP-Ribose) Polymerase-1 / genetics
  • Poly (ADP-Ribose) Polymerase-1 / metabolism*
  • Receptors, Androgen / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Tosyl Compounds / therapeutic use
  • Triple Negative Breast Neoplasms / drug therapy
  • Triple Negative Breast Neoplasms / genetics
  • Triple Negative Breast Neoplasms / metabolism*
  • Xenograft Model Antitumor Assays

Substances

  • Anilides
  • BRCA1 Protein
  • BRCA1 protein, human
  • Benzimidazoles
  • Nitriles
  • Receptors, Androgen
  • Tosyl Compounds
  • veliparib
  • bicalutamide
  • PARP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1