ArticleSteroids2014
From empirical to mechanism-based discovery of clinically useful Selective Estrogen Receptor Modulators (SERMs).
Article in Steroids, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed.
- Pharmacotherapeutic considerations of selective estrogen receptor modulators for vascular protection.Frontiers in pharmacology · 2026Review
- Development of NR0B2 as a therapeutic target for the re-education of tumor associated myeloid cells.Cancer letters · 2024Article
- Synthesis Studies and the Evaluation of CACS medicinal chemistry letters · 2024Article
- Estradiol and Mu opioid-mediated reward: The role of estrogen receptors in opioid use.Addiction neuroscience · 2023Article
- 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
- 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
- Article
- Insights into how phosphorylation of estrogen receptor at serine 305 modulates tamoxifen activity in breast cancer.Molecular and cellular endocrinology · 2019Review
- Is there a role for reproductive steroids in the etiology and treatment of affective disorders?Dialogues in clinical neuroscience · 2018Review
- The significance of cholesterol and its metabolite, 27-hydroxycholesterol in breast cancer.Molecular and cellular endocrinology · 2018Review
- Review
- Low-dose tamoxifen treatment in juvenile males has long-term adverse effects on the reproductive system: implications for inducible transgenics.Scientific reports · 2017Article
- A clinical guide to the management of genitourinary symptoms in breast cancer survivors on endocrine therapy.Therapeutic advances in medical oncology · 2017Review
- Novel Promising Estrogenic Receptor Modulators: Cytotoxic and Estrogenic Activity of Benzanilides and Dithiobenzanilides.PloS one · 2016Article
- Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research · 2015Article
- Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader.Endocrine-related cancer · 2015Article
- Estrogen receptors and their implications in colorectal carcinogenesis.Frontiers in oncology · 2015Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors.
Funding
Abstract
Our understanding of the molecular mechanisms underlying the pharmacological actions of estrogen receptor (ER) ligands has evolved considerably in recent years. Much of this knowledge has come from a detailed dissection of the mechanism(s) of action of the Selective Estrogen Receptor Modulators (SERMs) tamoxifen and raloxifene, drugs whose estrogen receptor (ER) agonist/antagonist properties are influenced by the cell context in which they operate. These studies have revealed that notwithstanding differences in drug pharmacokinetics, the activity of an ER ligand is determined primarily by (a) the impact that a given ligand has on the receptor conformation and (b) the ability of structurally distinct ER-ligand complexes to interact with functionally distinct coregulators. Exploitation of the established relationships between ER structure and activity has led to the development of improved SERMs with more favorable therapeutic properties and of tissue-selective estrogen complexes, drugs in which a SERM and an ER agonist are combined to yield a blended activity that results in distinct clinical profiles. Remarkably, endogenous ligands that exhibit SERM activity have also been identified. One of these ligands, 27-hydroxycholesterol (27HC), has been shown to manifest ER-dependent pathological activities in the cardiovascular system, bone and mammary gland. Whereas the physiological activity of 27HC remains to be determined, its discovery highlights how cells have adopted mechanisms to allow the same receptor ligand complex to manifest different activities in different cells, and also how these processes can be exploited for new drug development.
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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.