Effects of a combined treatment with GPR30 agonist G-1 and herceptin on growth and gene expression of human breast cancer cell lines

Cancer Invest. 2012 Jun;30(5):372-9. doi: 10.3109/07357907.2012.666690. Epub 2012 Apr 2.

Abstract

Expression of G-protein-coupled receptor 30 (GPR30) is present in HER2-overexpressing breast cancer. In this study, we examined to what extent GPR30-agonist G-1 would affect the antitumoral action of trastuzumab (Herceptin). Combined treatment with both drugs exerted an additive growth-inhibitory effect on breast cancer cells which was accompanied by a significant decline of cyclin A2 expression both on the protein and the mRNA level. Combined treatment also resulted in expression changes of c-fos, cyclin D1, or p21/WAF-1. The results of our study encourage further attempts to test the relevance of these in vitro data in the clinical setting.

MeSH terms

  • Antibodies, Monoclonal, Humanized / administration & dosage
  • Antibodies, Monoclonal, Humanized / pharmacology*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cyclopentanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Gene Expression Regulation / drug effects*
  • Genes, fos
  • Humans
  • Quinolines / pharmacology*
  • Receptors, Estrogen / agonists*
  • Receptors, G-Protein-Coupled / agonists*
  • Trastuzumab

Substances

  • 1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone
  • Antibodies, Monoclonal, Humanized
  • Cyclopentanes
  • GPER1 protein, human
  • Quinolines
  • Receptors, Estrogen
  • Receptors, G-Protein-Coupled
  • Trastuzumab