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Comparison of the Ligand Binding Specificity and Transcript Tissue Distribution of Estrogen Receptors α and β
Abstract
The rat estrogen receptor (ER) exists as two subtypes, ER alpha and ER beta, which differ in the C-terminal ligand binding domain and in the N-terminal transactivation domain. In this study we investigated the messenger RNA expression of both ER subtypes in rat tissues by RT-PCR and compared the ligand binding specificity of the ER subtypes. Saturation ligand binding analysis of in vitro synthesized human ER alpha and rat ER beta protein revealed a single binding component for 16 alpha-iodo-17 beta-estradiol with high affinity [dissociation constant (Kd) = 0.1 nM for ER alpha protein and 0.4 nM for ER beta protein]. Most estrogenic substances or estrogenic antagonists compete with 16 alpha-[125I]iodo-17 beta-estradiol for binding to both ER subtypes in a very similar preference and degree; that is, diethylstilbestrol > hexestrol > dienestrol > 4-OH-tamoxifen > 17 beta-estradiol > coumestrol, ICI-164384 > estrone, 17 alpha-estradiol > nafoxidine, moxestrol > clomifene > estriol, 4-OH-estradiol > tamoxifen, 2-OH-estradiol, 5-androstene-3 beta, 17 beta-diol, genistein for the ER alpha protein and dienestrol > 4-OH-tamoxifen > diethylstilbestrol > hexestrol > coumestrol, ICI-164384 > 17 beta-estradiol > estrone, genistein > estriol > nafoxidine, 5-androstene-3 beta, 17 beta-diol > 17 alpha-estradiol, clomifene, 2-OH-estradiol > 4-OH-estradiol, tamoxifen, moxestrol for the ER beta protein. The rat tissue distribution and/or the relative level of ER alpha and ER beta expression seems to be quite different, i.e. moderate to high expression in uterus, testis, pituitary, ovary, kidney, epididymis, and adrenal for ER alpha and prostate, ovary, lung, bladder, brain, uterus, and testis for ER beta. The described differences between the ER subtypes in relative ligand binding affinity and tissue distribution could contribute to the selective action of ER agonists and antagonists in different tissues.
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“which is one of the most potent EDCs on nuclear estrogen receptors (ERs), particularly ERβ (82, 83).”
From Endocrine Disruption of Vasopressin Systems and Related Behaviors (2017) · cites this paper as [83]
In the citing paper
“Soy and other legumes contain isoflavone phytoestrogens, which are used to aid in the recruitment of nitrogen-fixing bacteria but are also well-characterized xenoestrogens (83, 109, 110).”
From Endocrine Disruption of Vasopressin Systems and Related Behaviors (2017) · cites this paper as [83]
In the citing paper
“However, the ERβ receptors have a lower affinity for 17 β-estradiol relative to the ERα (14)”
From Sex Hormone Effects on Body Fluid Regulation (2008) · cites this paper as [14]
In the citing paper
“While both are present in mammals, beta receptors dominate in the gastrointestinal tract [67].”
From Phytoecdysteroids: Quantification in Selected Plant Species and Evaluation of Some Effects on Gastric Smooth Muscles (2024) · cites this paper as [67]
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Self-citation
Metadata
- Authors
- Kuiper, G. G. J. M., Carlsson, B., Grandien, K., Enmark, E., Häggblad, J., Nilsson, S., & Gustafsson, J.-A.
- Affiliations
- Karolinska Institutet (SE)
- Karo Pharma (Sweden) (SE)
- Department of KaroBio AB (B.C., J.H., S.N.) Huddinge, Sweden
- Center for Biotechnology and Department of Medical Nutrition, Karolinska Institute (G.G.J.M.K., K.G., E.E., J.-Å.G.) Huddinge, Sweden
- ORCID
- Grandien, Kaj
- Venue
- Endocrinology
- Publisher
- The Endocrine Society
- Published
- 1997-03-01
- Volume
- 138
- Issue
- 3
- Pages
- 863-870
- ISSN
- 0013-7227 (ISSN-L)
- 1945-7170
- OpenAlex
- W2073883348
- Cited by
- 4,442
- References
- 40
- Citations by year
- 2026: 35 · 2025: 49 · 2024: 56 · 2023: 56 · 2022: 53 · 2021: 92 · 2020: 86 · 2019: 103 · 2018: 89 · 2017: 104 · 2016: 103 · 2015: 122 · 2014: 160 · 2013: 176 · 2012: 148
- FWCI
- 118.20
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Effects and risks of endocrine disrupting chemicals
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- estrogen receptor alpha, estrogen receptor beta, ligand specificity, competitive binding, diethylstilbestrol, tamoxifen, genistein, rat tissues, estrogen receptor subtypes, transactivation domain
- MeSH terms
- Amino Acid Sequence, Animals, Female, Humans, Isomerism, Ligands, Male, Molecular Sequence Data, Receptors, Estrogen, RNA, Messenger, Tissue Distribution, Rats
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