ArticleMolecular endocrinology (Baltimore, Md.)2009
Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination.
Article in Molecular endocrinology (Baltimore, Md.), 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
30 citing papers in PubMed, 70 citations in OpenAlex.
- Bazedoxifene and Beyond: Identifying This SERM's Targets and Deciphering Its Molecular Mechanisms.Advances in pharmacological and pharmaceutical sciences · 2026Review
- Propolis mitigates histopathological alterations in the pituitary gland and reproductive system of female albino rats subjected to cadmium toxicity.Veterinary world · 2025Article
- Overcoming challenges in conducting early phase breast cancer prevention trials: Bazedoxifene and conjugated estrogens vs waitlist control.Contemporary clinical trials · 2024Article
- Estrone-mediated lowering of ROS and NOX4 improves endothelial function in ovariectomized wistar rats.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- Asymmetric allostery in estrogen receptor-α homodimers drives responses to the ensemble of estrogens in the hormonal milieu.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Anti-fibrotic effect of a selective estrogen receptor modulator in systemic sclerosis.Stem cell research & therapy · 2022Article
- Article
- The Trend in the Sales of Menopausal Hormone and Other Osteoporosis Medications in South Korea from 2016 to 2019.Journal of bone metabolism · 2021Article
- Sex Hormones in Lymphedema.Cancers · 2021Review
- Tissue-Selective Estrogen Complex and Breast.Journal of menopausal medicine · 2020Review
- Article
- Tissue selective estrogen complex (TSEC): a review.Menopause (New York, N.Y.) · 2018Review
- Estrogens Promote Misfolded Proinsulin Degradation to Protect Insulin Production and Delay Diabetes.Cell reports · 2018Article
- 27-Hydroxycholesterol Is an Estrogen Receptor β-Selective Negative Allosteric Modifier of 17β-Estradiol Binding.Endocrinology · 2018Article
- Article
- Clinical update on the use of ospemifene in the treatment of severe symptomatic vulvar and vaginal atrophy.International journal of women's health · 2016Review
- The Effect of Menopausal Hormone Therapies on Breast Cancer: Avoiding the Risk.Endocrinology and metabolism clinics of North America · 2015Review
- Breast-related effects of selective estrogen receptor modulators and tissue-selective estrogen complexes.Breast cancer research : BCR · 2014Review
- Treatment with bazedoxifene and conjugated estrogens results in regression of endometriosis in a murine model.Biology of reproduction · 2014Article
- Selective estrogen receptor modulators: tissue specificity and clinical utility.Clinical interventions in aging · 2014Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The use of estrogen-based therapies and the selective estrogen receptor (ER) modulator (SERM), raloxifene, which are approved for postmenopausal osteoporosis, is associated with side effects such as uterine/breast hyperproliferation, thromboembolism, and hot flashes. A combination of a new SERM, bazedoxifene (BZA), and Premarin (conjugated estrogens; CE) is under investigation to mitigate the estrogen/SERM side effects with promising results in Phase III clinical trials. To explore the mechanism of BZA/CE action, we investigated the recruitment of cofactor peptides to ERalpha by components of CE and a mixture containing the 10 major components of CE with or without three different SERMs. Here, we demonstrate differential recruitment of cofactor peptides to ERalpha by the individual CE components using a multiplex nuclear receptor-cofactor peptide interaction assay. We show that estrone and equilin are partial agonists in comparison with 17beta-estradiol in recruiting cofactor peptides to ERalpha. Further, CE was more potent than 17beta-estradiol in mediating ERalpha interaction with cofactor peptides. Interestingly, BZA was less potent than other SERMs in antagonizing the CE-mediated cofactor peptide recruitment to ERalpha. Finally, in accordance with these biochemical findings, 17beta-estradiol and CE, as well as SERM/CE combinations, showed differential gene regulation patterns in MCF-7 cells. In addition, BZA showed antagonism of a unique set of CE-regulated genes and did not down-regulate the expression of a number of CE-regulated genes, the expression of which was effectively antagonized by the other two SERMs. These results indicate that SERMs in combination with CE exhibit differential pharmacology, and therefore, combinations of other SERMs and estrogen preparations may not yield the same beneficial effects that are observed in clinic by pairing BZA with CE.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.