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
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Antibodies, Monoclonal, Humanized / administration & dosage
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Antibodies, Monoclonal, Humanized / pharmacology*
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Breast Neoplasms / drug therapy*
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cyclopentanes / pharmacology*
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Dose-Response Relationship, Drug
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Female
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Gene Expression Regulation / drug effects*
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Genes, fos
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Humans
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Quinolines / pharmacology*
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Receptors, Estrogen / agonists*
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Receptors, G-Protein-Coupled / agonists*
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Trastuzumab
Substances
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1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone
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Antibodies, Monoclonal, Humanized
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Cyclopentanes
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GPER1 protein, human
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Quinolines
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Receptors, Estrogen
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Receptors, G-Protein-Coupled
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Trastuzumab