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Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay
Published on: June 7, 2020
ERbeta: a novel estrogen receptor offers the potential for new drug development
S Nilsson1, G Kuiper, J A Gustafsson
1Karo Bio AB, Huddinge, Sweden.
Abstract:
There is increasing interest in developing better drugs for improving the health of women. Because of the multiple target organs for estrogens and the occurrence of both beneficial and unwanted effects during treatment, the key to improvement in drug therapy is the development of estrogen receptor modulators with better tissue selectivity. The recent discovery that there are not one but two estrogen receptors, ERalpha and ERbeta, each with its unique tissue distribution and with differing and sometimes opposing actions on certain genes, promises new hope for the development of novel, tissue-selective estrogens. Our present knowledge of the tissue distribution of ERalpha and ERbeta suggests that development of selective therapies for treatment and/or prevention of menopausal symptoms, osteoporosis, cardiovascular disease, type II diabetes, Alzheimer's disease and urinary incontinence is an achievable goal in the foreseeable future. Furthermore, it is possible that future estrogen therapy might be beneficial for men.
Insights
Developing selective estrogen therapies targeting estrogen receptors alpha and beta offers new hope for treating various conditions in women and potentially men. This approach aims to minimize unwanted side effects while maximizing benefits.
Area of Science:
- Endocrinology
- Pharmacology
- Women's Health
Background:
- Estrogen therapy presents challenges due to multiple target organs and side effects.
- Developing tissue-selective estrogen receptor modulators is crucial for improved drug therapy.
- The discovery of two distinct estrogen receptors, ERalpha and ERbeta, offers new therapeutic avenues.
Purpose of the Study:
- To explore the potential of novel, tissue-selective estrogens.
- To leverage the unique tissue distribution of ERalpha and ERbeta for targeted therapies.
- To identify future therapeutic applications for selective estrogen modulation.
Main Methods:
- Review of current knowledge on estrogen receptor (ERalpha and ERbeta) tissue distribution.
- Analysis of differing actions of ERalpha and ERbeta on specific genes.
- Evaluation of potential therapeutic targets based on receptor distribution.
Main Results:
- ERalpha and ERbeta exhibit distinct tissue distributions and actions.
- This distinctness provides a basis for developing tissue-selective estrogen therapies.
- Selective therapies show promise for conditions like menopausal symptoms, osteoporosis, cardiovascular disease, type II diabetes, Alzheimer's disease, and urinary incontinence.
Conclusions:
- Development of selective estrogen therapies targeting ERalpha and ERbeta is achievable.
- These therapies hold promise for treating a range of conditions in women.
- Potential benefits may extend to men as well.
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