Document Type
Article
Journal Title
Cell Death and Disease
Publication Date
Fall 10-17-2013
Volume
4
Abstract
The G-protein-coupled estrogen receptor 1 (GPER) has recently been reported to mediate the non-genomic action of estrogen in different types of cells and tissues. G-1 (1-[4-(6-bromobenzo[1,3] dioxol-5yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone) was developed as a potent and selective agonist for GPER. G-1 has been shown to induce the expression of genes and activate pathways that facilitate cancer cell proliferation by activating GPER. Here we demonstrate that G-1 has an anticancer potential with a mechanism similar to vinca alkaloids, the commonly used chemotherapy drugs. We found that G-1 blocks tubulin polymerization and thereby interrupts microtubule assembly in ovarian cancer cells leading to the arrest of cell cycle in the prophase of mitosis and the suppression of ovarian cancer cell proliferation. G-1 treatment also induces apoptosis of ovarian cancer cells. The ability of G-1 to target microtubules to suppress ovarian cancer cell proliferation makes it a promising candidate drug for treatment of ovarian cancer.
MeSH Headings
Animals, Apoptosis, Cell Line, Tumor, Cell Proliferation, Cyclopentanes, Female, Humans, Ovarian Neoplasms, Polymerization, Prophase, Quinolines, Receptors, Estrogen, Receptors, G-Protein-Coupled, Spindle Apparatus, Sus scrofa, Tubulin
DOI Link
ISSN
2041-4889
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.
Recommended Citation
Wang, Cheng; Lv, Xiangmin; He, Chunbo; Hua, G; Tsai, M-Y; and Davis, John S., "The G-protein-coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian cancer cells by blocking tubulin polymerization." (2013). Journal Articles: Obstetrics & Gynecology. 6.
https://digitalcommons.unmc.edu/com_obgyn_articles/6