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Updated: Apr 27, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential
Ilaria Paterni1, Carlotta Granchi1, John A Katzenellenbogen2
1Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Abstract:
Estrogen receptors alpha (ERα) and beta (ERβ) are nuclear transcription factors that are involved in the regulation of many complex physiological processes in humans. Modulation of these receptors by prospective therapeutic agents is currently being considered for prevention and treatment of a wide variety of pathological conditions, such as, cancer, metabolic and cardiovascular diseases, neurodegeneration, inflammation, and osteoporosis. This review provides an overview and update of compounds that have been recently reported as modulators of ERs, with a particular focus on their potential clinical applications.
Insights
Estrogen receptors alpha and beta (ERα and ERβ) regulate human physiology. This review updates compounds modulating ERs for treating diseases like cancer, metabolic disorders, and osteoporosis.
Area of Science:
- Endocrinology
- Molecular Biology
- Pharmacology
Background:
- Estrogen receptors alpha (ERα) and beta (ERβ) are key nuclear transcription factors.
- These receptors regulate numerous complex human physiological processes.
- Dysregulation of ER signaling is implicated in various diseases.
Purpose of the Study:
- To provide an overview of recent ER modulators.
- To update knowledge on compounds targeting ERα and ERβ.
- To focus on the clinical applications of these modulators.
Main Methods:
- Literature review of recent scientific publications.
- Analysis of identified ER modulators.
- Assessment of potential therapeutic applications.
Main Results:
- Identification of novel compounds modulating ERα and ERβ.
- Summary of recent advancements in ER modulator research.
- Evaluation of therapeutic potential across diverse pathological conditions.
Conclusions:
- ER modulators show promise for treating cancer, metabolic, cardiovascular, and neurodegenerative diseases.
- Further research into ER modulation is crucial for clinical applications.
- Targeting ERs offers a potential therapeutic strategy for multiple human diseases.
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