scholarly journals Novel drugs that target the estrogen-related receptor alpha: their therapeutic potential in breast cancer

2014 ◽  
pp. 225 ◽  
Author(s):  
Felicity May
Keyword(s):  
Breast Cancer ◽  
Therapeutic Potential ◽  
Receptor Alpha ◽  
Novel Drugs ◽  
Estrogen Related Receptor

scholarly journals MiR-137 Targets Estrogen-Related Receptor Alpha and Impairs the Proliferative and Migratory Capacity of Breast Cancer Cells

PLoS ONE ◽  
2012 ◽  
Vol 7 (6) ◽  
pp. e39102 ◽  
Author(s):  
Yuanyin Zhao ◽  
Yuping Li ◽  
Guiyu Lou ◽  
Li Zhao ◽  
Zhizhen Xu ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Receptor Alpha ◽  
Migratory Capacity ◽  
Estrogen Related Receptor

scholarly journals Development of Novel Cell Lines for High-Throughput Screening to Detect Estrogen-Related Receptor Alpha Modulators

2017 ◽  
Vol 22 (6) ◽  
pp. 720-731 ◽  
Author(s):  
Christina T. Teng ◽  
Jui-Hua Hsieh ◽  
Jinghua Zhao ◽  
Ruili Huang ◽  
Menghang Xia ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
High Throughput ◽  
High Throughput Screening ◽  
Environmental Chemicals ◽  
Screening Tools ◽  
Receptor Alpha ◽  
Pharmacologically Active ◽  
Estrogen Related Receptor

Estrogen-related receptor alpha (ERRα), the first orphan nuclear receptor discovered, is crucial for the control of cellular energy metabolism. ERRα and its coactivator, peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), are required for rapid energy production in response to environmental challenges. They have been implicated in the etiology of metabolic disorders such as type 2 diabetes and metabolic syndrome. ERRα also plays a role in the pathogenesis of breast cancer. Identification of compounds that modulate ERRα signaling may elucidate environmental factors associated with these diseases. Therefore, we developed stable cell lines containing an intact ERRα signaling pathway, with and without the coactivator PGC-1α, to use as high-throughput screening tools to detect ERRα modulators. The lentiviral PGC-1α expression constructs and ERRα multiple hormone response element (MHRE) reporters were introduced into HEK293T cells that express endogenous ERRα. A cell line expressing the reporter alone was designated “ERR.” A second cell line expressing both reporter and PGC-1α was named “PGC/ERR.” Initial screenings of the Library of Pharmacologically Active Compounds (LOPAC) identified 33 ERR and 22 PGC/ERR agonists, and 54 ERR and 15 PGC/ERR antagonists. Several potent ERRα agonists were dietary plant compounds (e.g., genistein). In conclusion, these cell lines are suitable for high-throughput screens to identify environmental chemicals affecting metabolic pathways and breast cancer progression.

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