NDLI: The G-protein-coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian cancer cells by blocking tubulin polymerization.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Wang, C. Lv, X. He, C. Hua, G. Tsai, M-Y Davis, J. S.
Description	Country affiliation: United States Author Affiliation: Wang C ( 1] Olson Center for Women's Health, University of Nebraska Medical Center, Omaha, NE, USA [2] Departments of Obstetrics and Gynecology, University of Nebraska Medical Center, Omaha, NE, USA [3] Fred and Pamela Buffet Cancer Center, University of Nebraska Medical Center, Omaha, NE, USA.)
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.
File Format	HTM / HTML
e-ISSN	20414889
DOI	10.1038/cddis.2013.397
Journal	Cell Death and Disease
Volume Number	4
Language	English
Publisher	Nature Publishing Group
Publisher Date	2013-10-17
Publisher Place	Great Britain (UK)
Access Restriction	Open
Subject Keyword	Quinolines Research Support, N.i.h., Extramural Research Support, Non-u.s. Gov't Cell Proliferation Spindle Apparatus Tubulin Ovarian Neoplasms Cyclopentanes Research Support, U.s. Gov't, Non-p.h.s. Receptors, Estrogen Prophase Polymerization Receptors, G-protein-coupled Pharmacology Metabolism Drug Effects Discipline Cell Biology Pathology Animals Cell Line, Tumor Sus Scrofa Agonists Apoptosis
Content Type	Text
Resource Type	Article

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