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Updated: Aug 17, 2026

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause
Published on: August 13, 2019
Recent advances in estrogen receptor modulators
1GlaxoSmithKline Inc, Metabolic and Viral Diseases Drug Discovery, Research Triangle Park, PO Box 13398, NC 27705, USA. brad.r.henke@gsk.com
Abstract:
Modulation of estrogen action is an effective treatment for alleviating the symptoms associated with menopause, and also provides an alternative to ablative surgery for the treatment of breast cancer. The side effects associated with the currently used estrogen receptor-modulating drugs have resulted in the pursuit of agents with an improved therapeutic profile. Recent advances in understanding the molecular determinants of estrogen receptor signaling have contributed to the continued discovery and development of novel chemical compounds designed to exploit this knowledge. This review focuses on the recent clinical and preclinical development of novel classes of ligands that modulate the two estrogen receptor subtypes.
Insights
New estrogen receptor modulators offer improved treatments for menopause and breast cancer, addressing side effects of current drugs. Research focuses on novel ligands targeting estrogen receptor subtypes for better therapeutic outcomes.
Area of Science:
- Endocrinology
- Pharmacology
- Oncology
Background:
- Estrogen modulation effectively treats menopause symptoms and breast cancer.
- Current estrogen receptor drugs have significant side effects.
- Understanding estrogen receptor signaling drives new drug discovery.
Purpose of the Study:
- To review recent clinical and preclinical developments in novel estrogen receptor modulators.
- To highlight new ligand classes targeting estrogen receptor subtypes.
Main Methods:
- Review of recent clinical and preclinical studies.
- Analysis of novel chemical compounds targeting estrogen receptor subtypes.
Main Results:
- Emerging novel classes of ligands demonstrate potential for improved estrogen modulation.
- Advances in understanding estrogen receptor signaling facilitate targeted drug development.
Conclusions:
- Novel estrogen receptor ligands are being developed with improved therapeutic profiles.
- Targeted modulation of estrogen receptor subtypes offers promising therapeutic strategies.
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