ArticleMolecular endocrinology (Baltimore, Md.)2012
Research resource: Transcriptional profiling in a cellular model of breast cancer reveals functional and mechanistic differences between clinically relevant SERM and between SERM/estrogen complexes.
Article in Molecular endocrinology (Baltimore, Md.), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
What it found
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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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Who cites it
33 citing papers in PubMed, 59 citations in OpenAlex.
- Bazedoxifene and Beyond: Identifying This SERM's Targets and Deciphering Its Molecular Mechanisms.Advances in pharmacological and pharmaceutical sciences · 2026Review
- 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
- The Liver X Receptor Is Selectively Modulated to Differentially Alter Female Mammary Metastasis-associated Myeloid Cells.Endocrinology · 2022Article
- Our evolving understanding of how 27-hydroxycholesterol influences cancer.Biochemical pharmacology · 2022Review
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- Article
- Estrogen and sex-dependent loss of the vocal learning system in female zebra finches.Hormones and behavior · 2021Article
- G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer.Breast cancer research and treatment · 2020Article
- Translational offsetting as a mode of estrogen receptor α-dependent regulation of gene expression.The EMBO journal · 2019Article
- Role of SUMOylation in differential ERα transcriptional repression by tamoxifen and fulvestrant in breast cancer cells.Oncogene · 2019Article
- Review
- The Roles of Cholesterol and Its Metabolites in Normal and Malignant Hematopoiesis.Frontiers in endocrinology · 2019Review
- Effect of a tissue selective estrogen complex on breast cancer: Role of unique properties of conjugated equine estrogen.International journal of cancer · 2018Article
- Transcriptomic response of breast cancer cells to anacardic acid.Scientific reports · 2018Article
- 17Journal of the Endocrine Society · 2018Article
- 27-Hydroxycholesterol induces hematopoietic stem cell mobilization and extramedullary hematopoiesis during pregnancy.The Journal of clinical investigation · 2017Article
- Antiestrogens: structure-activity relationships and use in breast cancer treatment.Journal of molecular endocrinology · 2017Review
- Estrogen receptor-α and aryl hydrocarbon receptor involvement in the actions of botanical estrogens in target cells.Molecular and cellular endocrinology · 2016Article
- Effect of Novel Melanocortin Type 2 Receptor Antagonists on the Corticosterone Response to ACTH in the Neonatal Rat Adrenal Gland In Vivo and In Vitro.Frontiers in endocrinology · 2016Article
- Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader.Endocrine-related cancer · 2015Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Exploitation of the relationship between estrogen receptor (ER) structure and activity has led to the development of 1) selective ER modulators (SERM), compounds whose relative agonist/antagonist activities differ between target tissues; 2) selective ER degraders (SERD), compounds that induce a conformational change in the receptor that targets it for proteasomal degradation; and 3) tissue-selective estrogen complexes (TSEC), drugs in which a SERM and an ER agonist are combined to yield a blended activity that results in distinct clinical profiles. In this study, we have performed a comprehensive head-to-head analysis of the transcriptional activity of these different classes of ERM in a cellular model of breast cancer. Not surprisingly, these studies highlighted important functional differences and similarities among the existing SERM, selective ER degraders, and TSEC. Of particular importance was the identification of genes that were regulated by various TSEC combinations but not by an estrogen or SERM alone. Cumulatively, the findings of this analysis are informative with respect to the mechanisms by which ER is engaged by different enhancers/promoters and highlights how promoter context influences the pharmacological activity of ER ligands.
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Registered trials
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.