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Related Experiment Video

Updated: May 29, 2026

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause

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Published on: August 13, 2019

Development of subtype-selective oestrogen receptor-based therapeutics.

Stefan Nilsson¹, Konrad F Koehler, Jan-Åke Gustafsson

¹Karo Bio AB, Novum, SE-141 57 Huddinge, Sweden.

Nature Reviews. Drug Discovery

|September 17, 2011

Summary

Selective oestrogen receptor modulators targeting oestrogen receptor-alpha or oestrogen receptor-beta offer a more optimal approach for treating diseases. These subtype-selective ligands show promise for various conditions, including cancer and neurodegenerative disorders.

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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer

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Published on: March 17, 2016

Area of Science:

Endocrinology and molecular biology
Cellular signaling pathways
Gene expression regulation

Background:

Oestrogen receptors (ERs), specifically ER-α and ER-β, are key regulators of cellular processes.
Their activity is vital for development, homeostasis, and managing various diseases.
Current therapies utilize non-selective ER modulators with established efficacy.

Purpose of the Study:

To explore the potential of subtype-selective oestrogen receptor modulators.
To investigate targeted therapies for conditions like cancer, cardiovascular disease, multiple sclerosis, and Alzheimer's disease.
To highlight the advantages of targeting ER-α or ER-β specifically.

Main Methods:

Review of existing literature on oestrogen receptor subtypes and modulators.
Analysis of emerging data on subtype-selective ligand development.
Comparative assessment of classical versus subtype-selective therapeutic strategies.

Main Results:

Emerging data indicate that subtype-selective ligands offer a more precise therapeutic approach.
Targeting ER-α or ER-β specifically may lead to improved treatment outcomes.
Potential applications span oncology, cardiovascular health, and neurological disorders.

Conclusions:

Development of subtype-selective oestrogen receptor modulators represents a promising advancement in therapeutic strategies.
Targeted modulation of ER-α or ER-β could optimize treatment for a range of complex diseases.
Further research into these selective ligands is warranted for clinical application.