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

ISSN

2041-4889

Creative Commons License


This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.

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