Glucose-dependent GPER1 expression modulates tamoxifen-induced IGFBP-1 accumulation
1Department of Chemistry and Biochemistry, New Mexico State University, Las Cruces, New Mexico, USA.
Journal of Molecular Endocrinology
|June 27, 2019
Summary
Low glucose levels increase G protein-coupled estrogen receptor 1 (GPER1) expression in breast cancer cells, mediated by AMP-activated protein kinase (AMPK). This enhances tamoxifen
Area of Science:
- Endocrinology
- Molecular Biology
- Cancer Research
Background:
- G protein-coupled estrogen receptor 1 (GPER1) mediates rapid estrogen signaling.
- GPER1's role in hormone-responsive cancers is known, but its expression regulation is unclear.
- Understanding GPER1 regulation is crucial for breast cancer therapy, including tamoxifen action.
Purpose of the Study:
- To investigate the effect of D-glucose levels on GPER1 expression in breast cancer cells.
- To determine the role of AMP-activated protein kinase (AMPK) in glucose-mediated GPER1 regulation.
- To assess if altered GPER1 expression impacts tamoxifen's efficacy in breast cancer cells.
Main Methods:
- Culturing breast cancer cells in varying D-glucose concentrations.
- Utilizing small molecule modulators and genetic manipulation of AMPK.
- Measuring GPER1 expression and tamoxifen-induced IGFBP-1 transcription.
Main Results:
- Low D-glucose significantly increased GPER1 expression in breast cancer cells.
- AMPK activation promoted GPER1 accumulation, while inhibition reduced it under low glucose.
- D-glucose deprivation enhanced GPER1-mediated tamoxifen-induced IGFBP-1 transcription.
Conclusions:
- GPER1 expression is regulated by D-glucose levels in breast cancer cells.
- AMPK is a key mediator in the glucose-dependent regulation of GPER1.
- Altered GPER1 expression due to glucose availability may influence breast cancer cell sensitivity to tamoxifen.
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