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Updated: Mar 6, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
Estrogen receptor agonists/antagonists in breast cancer therapy: A critical review
A Jameera Begam1, S Jubie1, M J Nanjan2
1Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Udhagamandalam, India; A Constituent College of JSS University, Mysore, India.
Abstract:
Estrogens display intriguing tissue selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer. There are also strong evidences to show that both endogenous and exogenous estrogens are involved in the pathogenesis of breast cancer. Tamoxifen has been the only drug of choice for more than 30years to treat patients with estrogen related (ER) positive breast tumors. There is a need therefore, for identifying newer, potential and novel candidates for breast cancer. Keeping this in view, the present review focuses on selective estrogen receptor modulators and estrogen antagonists such as sulfatase and aromatase inhibitors involved in breast cancer therapy. A succinct and critical overview of the structure of estrogen receptors, their signaling and involvement in breast carcinogenesis are herein described.
Insights
Newer breast cancer therapies are needed as Tamoxifen is the sole option for estrogen-related tumors. This review explores selective estrogen receptor modulators and antagonists for improved breast cancer treatment.
Area of Science:
- Oncology
- Endocrinology
- Pharmacology
Background:
- Estrogen's tissue-selective actions are crucial for breast cancer therapeutics.
- Estrogens, both endogenous and exogenous, play a role in breast cancer development.
- Tamoxifen has been the primary treatment for estrogen receptor-positive breast tumors for over 30 years.
Purpose of the Study:
- To review novel therapeutic candidates for breast cancer.
- To focus on selective estrogen receptor modulators and estrogen antagonists.
- To provide an overview of estrogen receptors, signaling, and their role in breast carcinogenesis.
Main Methods:
- Literature review of selective estrogen receptor modulators.
- Analysis of estrogen antagonists, including sulfatase and aromatase inhibitors.
- Critical overview of estrogen receptor structure and signaling pathways.
Main Results:
- Identified selective estrogen receptor modulators and antagonists as key therapeutic targets.
- Highlighted the involvement of estrogen receptor signaling in breast cancer.
- Discussed the limitations of current therapies and the need for novel agents.
Conclusions:
- Selective estrogen receptor modulators and antagonists offer promising avenues for breast cancer therapy.
- Understanding estrogen receptor signaling is vital for developing effective breast cancer treatments.
- There is a significant need for novel therapeutic strategies beyond Tamoxifen for estrogen-related breast cancers.
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