Cyclohexylpiperazine derivative PB28, a σ2 agonist and σ1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer

@article{Azzariti2006CyclohexylpiperazineDP,
  title={Cyclohexylpiperazine derivative PB28, a $\sigma$2 agonist and $\sigma$1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer},
  author={Amalia Azzariti and Nicola Antonio Colabufo and Francesco Berardi and Letizia Porcelli and Mauro Niso and Grazia Maria Simone and Roberto Perrone and Angelo Virgilio Paradiso},
  journal={Molecular Cancer Therapeutics},
  year={2006},
  volume={5},
  pages={1807 - 1816}
}
σ Ligands have recently been shown to have cytotoxic activity, to induce ceramide-dependent/caspase-independent apoptosis, and to down-regulate P-glycoprotein (P-gp) mRNA levels in some mouse and human models. In this study, we verified whether a mixed σ2 agonist/σ1 antagonist, PB28, was able to have antitumor activity and to enhance anthracycline efficacy in two human breast cancer cell lines, MCF7 and MCF7 ADR, both characterized by significant σ2 receptor expression, by high and low σ1… 

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