Dual suppression of estrogenic and inflammatory activities for targeting of endometriosis
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The estrogen-dependent inflammatory and neuroangiogenic activities that drive endometriosis can be suppressed by estrogen receptor ligands in mice.
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ESR2 ligands acting as estrogen antagonists in endometriotic tissue show promising results in murine models.
“ESR2 ligands acting as estrogen antagonists in endometriotic tissue show promising results in murine models and should also be considered as potential therapeutics (Zhao et al., 2015).”
From Endometriosis and nuclear receptors (2019) · cites this paper as Zhao et al., 2015
The Results section (page unavailable) reports that CLI acts predominantly through ERβ (ESR2) and suppresses endometriotic lesions in mice, supporting the therapeutic promise described. But the paper’s other tested ligand, OBHS, acts predominantly through ERα, so the evidence does not establish the same result for multiple ESR2-directed ligands. (LLM, conf=0.86)
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- Authors
- Zhao, Y., Gong, P., Chen, Y., Nwachukwu, J. C., Srinivasan, S., Ko, C., Bagchi, M. K., Taylor, R. N., Korach, K. S., Nettles, K. W., Katzenellenbogen, J. A., & Katzenellenbogen, B. S.
- Affiliations
- University of Illinois Urbana-Champaign (US)
- Scripps Research Institute (US)
- Wake Forest University Health Sciences (US)
- National Institute of Environmental Health Sciences (US)
- Corresponding author
- Katzenellenbogen, Benita S.
- ORCID
- Venue
- Science Translational Medicine
- Published
- 2015-01-21
- Volume
- 7
- Issue
- 271
- Pages
- 271ra9-271ra9
- ISSN
- 1946-6234 (ISSN-L)
- 1946-6242
- PMC
- PMC4790140
- OpenAlex
- W2152982261
- Cited by
- 170
- References
- 47
- Citations by year
- 2026: 10 · 2025: 16 · 2024: 18 · 2023: 11 · 2022: 14 · 2021: 9 · 2020: 15 · 2019: 17 · 2018: 18 · 2017: 12 · 2016: 19 · 2015: 11
- FWCI
- 22.82
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Science Translational Medicine (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- NIH (U54 HD055787, PHS 5R01DK015556, 5R01DK077085)
- Frenchman's Creek Women for Cancer Research
- Topics
- Health Sciences › Medicine › Reproductive Medicine › Endometriosis Research and Treatment
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Effects and risks of endocrine disrupting chemicals
- Keywords
- endometriosis, estrogen receptor ligands, estrogen receptor alpha, estrogen receptor beta, anti-inflammatory activity, angiogenesis, neurogenesis, endometriotic stromal cells, fertility preservation
- MeSH terms
- Letrozole, Animals, Anti-Inflammatory Agents, Cell Survival, Cells, Cultured, Disease Models, Animal, Drug Therapy, Combination, Endometriosis, Estrogens, Female, Fertility, Humans, Indazoles, Inflammation, Ligands, Macrophages, Mice, Inbred C57BL, Mice, Transgenic, Neurons, Nitriles, Receptors, Estrogen, Triazoles, Treatment Outcome, Stromal Cells, Disease Progression, Embryonic Stem Cells
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