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G-1 Inhibits Breast Cancer Cell Growth via Targeting Colchicine-Binding Site of Tubulin to Interfere with Microtubule Assembly
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Abstract
G-protein–coupled estrogen receptor 1 (GPER1) has been reported to play a significant role in mediating the rapid estrogen actions in a wide range of normal and cancer cells. G-1 was initially developed as a selective agonist for GPER. However, the molecular mechanisms underlying the actions of G-1 are unknown, and recent studies report inconsistent effects of G-1 on the growth of breast cancer cells. By employing high-resolution laser scanning confocal microscopy and time-lapse imaging technology, as well as biochemical analyses, in the current study, we provide convincing in vitro and in vivo evidence that G-1 is able to suppress the growth of breast cancer cells independent of the expression status of GPERs and classic estrogen receptors. Interestingly, we found that triple-negative breast cancer cells (TNBC) are very sensitive to G-1 treatment. We found that G-1 arrested the cell cycle in the prophase of mitosis, leading to caspase activation and apoptosis of breast cancer cells. Our mechanistic studies indicated that G-1, similar to colchicine and 2-methoxyestradiol, binds to colchicine binding site on tubulin, inhibiting tubulin polymerization and subsequent assembly of normal mitotic spindle apparatus during breast cancer cell mitosis. Therefore, G-1 is a novel microtubule-targeting agent and could be a promising anti-microtubule drug for breast cancer treatment, especially for TNBC treatment. Mol Cancer Ther; 16(6); 1080–91. ©2017 AACR.
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“Both fostamatinib and colchicine have shown antitumor and anti-metastasis effects in animal models of breast cancer34,35.”
From ASGARD is a single-cell guided pipeline to aid repurposing of drugs (2023) · cites this paper as [34]
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Microtubules as a target for anticancer drugs
Jordan, M. A., & Wilson, L. (2004) · Nature Reviews Cancer · doi:10.1038/nrc1317 · Cited by 4,000
A transmembrane intracellular estrogen receptor mediates rapid cell signaling
Revankar, C. M., Cimino, D. F., Sklar, L. A., Arterburn, J. B., & Prossnitz, E. R. (2005) · Science · doi:10.1126/science.1106943 · Cited by 2,302
Caspase-3 Is Required for DNA Fragmentation and Morphological Changes Associated with Apoptosis
Jänicke, R. U., Sprengart, M. L., Wati, M. R., & Porter, A. G. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.16.9357 · Cited by 1,955
Estrogen Carcinogenesis in Breast Cancer
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Microtubule-binding agents: a dynamic field of cancer therapeutics
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Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells
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Self-citationThe G-protein-coupled estrogen receptor GPER in health and disease
Prossnitz, E. R., & Barton, M. (2011) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2011.122 · Cited by 925 · cited 2×
“Since its first report in 2006, G-1 has been wildly used to investigate the functions of GPER in various tissues and organs (4).”
BackgroundFilardo, E. J., Quinn, J. A., Frackelton, A. R., & Bland, K. I. (2002) · Molecular Endocrinology · doi:10.1210/mend.16.1.0758 · Cited by 907
Virtual and biomolecular screening converge on a selective agonist for GPR30
Bologa, C., Revankar, C. M., Young, S. M., Edwards, B. S., Arterburn, J. B., Kiselyov, A. S., Parker, M. A., Tkachenko, S. E., Savchuk, N., Sklar, L. A., et al. (2006) · Nature Chemical Biology · doi:10.1038/nchembio775 · Cited by 819
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Hernández-Silva, C. D., Villegas-Pineda, J. C., & Pereira-Suárez, A. L. (2020) · Frontiers in Endocrinology · doi:10.3389/fendo.2020.00544 · Cited by 74
ASGARD is a single-cell guided pipeline to aid repurposing of drugs
He, B., Xiao, Y., Liang, H., Huang, Q., Du, Y., Li, Y., Garmire, D., Sun, D., & Garmire, L. X. (2023) · Nature Communications · doi:10.1038/s41467-023-36637-3 · Cited by 57
Metadata
- Authors
- Lv, X., He, C., Huang, C., Hua, G., Wang, Z., Remmenga, S. W., Rodabough, K. J., Karpf, A. R., Dong, J., Davis, J. S., & Wang, C.
- Affiliations
- University of Nebraska Medical Center (US)
- Huazhong Agricultural University (CN)
- First Affiliated Hospital of Zhengzhou University (CN)
- Fred and Pamela Buffett Cancer Center (US)
- Omaha VA Medical Center (US)
- Corresponding author
- Wang, Cheng
- ORCID
- Venue
- Molecular Cancer Therapeutics
- Published
- 2017-06-01
- Volume
- 16
- Issue
- 6
- Pages
- 1080-1091
- ISSN
- 1535-7163 (ISSN-L)
- 1538-8514
- PMC
- PMC5457708
- OpenAlex
- W2592111594
- Cited by
- 53
- References
- 50
- Citations by year
- 2026: 3 · 2025: 4 · 2024: 8 · 2023: 9 · 2022: 9 · 2021: 7 · 2020: 4 · 2019: 6 · 2018: 3
- FWCI
- 2.04
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Molecular Cancer Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- U.S. Department of Veterans Affairs (I01 BX000512)
- National Cancer Institute (R01CA201500, R01CA197976)
- National Institute of General Medical Sciences (P30GM106397, R01GM109066)
- Eunice Kennedy Shriver National Institute of Child Health and Human Development (R00HD059985)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Microtubule and mitosis dynamics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Keywords
- G-1, G protein-coupled estrogen receptor, breast cancer, triple-negative breast cancer, colchicine binding site, tubulin, microtubule assembly, mitotic spindle, mitotic arrest, apoptosis, caspase activation, 2-methoxyestradiol
- MeSH terms
- Animals, Antineoplastic Agents, Binding Sites, Cell Cycle, Cyclopentanes, Disease Models, Animal, Female, Humans, Microtubules, Protein Binding, Quinolines, Receptors, Estrogen, Tubulin, Apoptosis, Xenograft Model Antitumor Assays, Cell Line, Tumor, Cell Proliferation, Tubulin Modulators, Mice, Protein Multimerization
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