Targeting PSG1 to enhance chemotherapeutic efficacy: new application for anti-coagulant the dicumarol

Clin Sci (Lond). 2016 Dec 1;130(24):2267-2276. doi: 10.1042/CS20160536. Epub 2016 Sep 21.

Abstract

Chemotherapeutic response is critical for the successful treatment and good prognosis in cancer patients. In this study, we analysed the gene expression profiles of preoperative samples from oestrogen receptor (ER)-negative breast cancer patients with different responses to taxane-anthracycline-based (TA-based) chemotherapy, and identified a group of genes that was predictive. Pregnancy specific beta-1-glycoprotein 1 (PSG1) played a central role within signalling pathways of these genes. Inhibiting PSG1 can effectively reduce chemoresistance via a transforming growth factor-β (TGF-β)-related pathway in ER-negative breast cancer cells. Drug screening then identified dicumarol (DCM) to target the PSG1 and inhibit chemoresistance to TA-based chemotherapy in vitro, in vivo, and in clinical samples. Taken together, this study highlights PSG1 as an important mediator of chemoresistance, whose effect could be diminished by DCM.

Keywords: chemoresistance; dicumarol; pregnancy specific beta-1-glycoprotein 1 (PSG1).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticoagulants / therapeutic use*
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / genetics*
  • Breast Neoplasms / metabolism
  • Bridged-Ring Compounds / therapeutic use
  • Cell Line, Tumor
  • Dicumarol / therapeutic use*
  • Drug Resistance, Neoplasm
  • Female
  • Humans
  • Pregnancy-Specific beta 1-Glycoproteins / antagonists & inhibitors*
  • Pregnancy-Specific beta 1-Glycoproteins / genetics
  • Pregnancy-Specific beta 1-Glycoproteins / metabolism
  • Taxoids / therapeutic use
  • Transforming Growth Factor beta / genetics
  • Transforming Growth Factor beta / metabolism

Substances

  • Anticoagulants
  • Bridged-Ring Compounds
  • Pregnancy-Specific beta 1-Glycoproteins
  • Taxoids
  • Transforming Growth Factor beta
  • taxane
  • Dicumarol