Birinapant (TL32711) Improves Responses to GEM/AZD7762 Combination Therapy in Triple-negative Breast Cancer Cell Lines

Anticancer Res. 2016 Jun;36(6):2649-57.

Abstract

Background: Triple-negative breast cancer (TNBC) is an aggressive form of breast cancer currently lacking targeted therapies. Our previous work demonstrated a therapeutic synergism with gemcitabine (GEM) and the CHK1 inhibitor (AZD7762) combination treatment in a TNBC cell line. We hypothesized that the response to this combination therapy would differ among heterogeneous TNBC patients and that addition of a SMAC mimetic (TL32711) could improve efficacy.

Materials and methods: Therapeutic responses to GEM, GEM/AZD7762, and GEM/AZD7762/TL32711 combinations were investigated by XTT assays and western blotting of cell cycle and apoptosis-related proteins in ten TNBC cell lines.

Results: TNBC cell lines harboring low levels of endogenous CHK1, cIAP1 and cIAP2 were responsive to GEM alone, whereas cell lines demonstrating a minimal increase in phospho-S345 CHK1 after treatment were responsive to GEM/AZD7762 or GEM/AZD7762/TL32711 combination.

Conclusion: The response of TNBC cells to particular therapies varies and will require development of predictive biomarkers.

Keywords: CHK1; Combination treatment; TL32711; triple-negative breast cancer.

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Checkpoint Kinase 1 / metabolism
  • DNA Repair
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives*
  • Dipeptides / administration & dosage*
  • Female
  • Gemcitabine
  • Humans
  • Indoles / administration & dosage*
  • Phosphorylation
  • Thiophenes / administration & dosage*
  • Triple Negative Breast Neoplasms / drug therapy*
  • Triple Negative Breast Neoplasms / pathology
  • Urea / administration & dosage
  • Urea / analogs & derivatives*

Substances

  • 3-(carbamoylamino)-5-(3-fluorophenyl)-N-(3-piperidyl)thiophene-2-carboxamide
  • Dipeptides
  • Indoles
  • Thiophenes
  • Deoxycytidine
  • birinapant
  • Urea
  • CHEK1 protein, human
  • Checkpoint Kinase 1
  • Gemcitabine