Title |
MIBE acts as antagonist ligand of both estrogen receptor α and GPER in breast cancer cells
|
---|---|
Published in |
Breast Cancer Research, January 2012
|
DOI | 10.1186/bcr3096 |
Pubmed ID | |
Authors |
Rosamaria Lappano, Maria Francesca Santolla, Marco Pupo, Maria Stefania Sinicropi, Anna Caruso, Camillo Rosano, Marcello Maggiolini |
Abstract |
The multiple biological responses to estrogens are mainly mediated by the classical estrogen receptors ERα and ERβ, which act as ligand-activated transcription factors. ERα exerts a main role in the development of breast cancer; therefore, the ER antagonist tamoxifen has been widely used although its effectiveness is limited by de novo and acquired resistance. Recently, GPR30/GPER, a member of the seven-transmembrane G protein-coupled receptor family, has been implicated in mediating the effects of estrogens in various normal and cancer cells. In particular, GPER triggered gene expression and proliferative responses induced by estrogens and even ER antagonists in hormone-sensitive tumor cells. Likewise, additional ER ligands showed the ability to bind to GPER eliciting promiscuous and, in some cases, opposite actions through the two receptors. We synthesized a novel compound (ethyl 3-[5-(2-ethoxycarbonyl-1-methylvinyloxy)-1-methyl-1H-indol-3-yl]but-2-enoate), referred to as MIBE, and investigated its properties elicited through ERα and GPER in breast cancer cells. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 1 | 25% |
Italy | 1 | 25% |
Unknown | 2 | 50% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 3 | 75% |
Practitioners (doctors, other healthcare professionals) | 1 | 25% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
India | 1 | 2% |
Unknown | 54 | 98% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 13 | 24% |
Student > Master | 7 | 13% |
Student > Postgraduate | 5 | 9% |
Professor | 4 | 7% |
Researcher | 4 | 7% |
Other | 11 | 20% |
Unknown | 11 | 20% |
Readers by discipline | Count | As % |
---|---|---|
Agricultural and Biological Sciences | 14 | 25% |
Biochemistry, Genetics and Molecular Biology | 10 | 18% |
Pharmacology, Toxicology and Pharmaceutical Science | 6 | 11% |
Medicine and Dentistry | 5 | 9% |
Chemistry | 2 | 4% |
Other | 5 | 9% |
Unknown | 13 | 24% |