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Target intelligence / Profile preview
Estrogen Receptor Alpha (ERα)
- Target
- ERα
- Molecular classification
- Nuclear hormone receptor, Transcription factor, Receptor
01
Overview
Estrogen receptor alpha (ERα) is a nuclear hormone receptor and transcription factor that mediates cellular responses to estrogens. It plays critical roles in reproductive system development and function, bone density regulation, metabolic homeostasis, cardiovascular protection, and modulation of inflammatory processes. ERα dysregulation is implicated in various diseases, including breast cancer, ovarian cancer, prostate cancer, metabolic disorders, and cardiovascular disease. It is a key therapeutic target, particularly in ER-positive breast cancer.
- Other names
- ER-alphaNR3A1Estrogen receptor 1ESR1
02
Mechanism of action
Ligand-dependent nuclear transcription factor; upon binding estrogen ligands, ERα dimerizes and translocates to the nucleus where it binds EREs on target genes or interacts with other transcription factors. Also mediates rapid non-genomic signaling.
03
Biological functions
Gene transcription regulationReproductive system development and functionBone density regulationMetabolic homeostasisCardiovascular protectionModulation of inflammatory processesSignal transduction
04
Disease associations
Breast cancerOvarian cancerProstate cancerMetabolic disordersCardiovascular disease
05
Safety considerations
Feminizing side effects in menIncreased risk of thromboembolic eventsEndometrial cancer risk (with some SERMs)
06
Interacting drugs
Tamoxifen
2 more in the full profile.
07
Biomarkers
ERα expression level in breast cancer tissue (for treatment selection)
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