ArticleJournal of medicinal chemistry2015
Highly selective salicylketoxime-based estrogen receptor β agonists display antiproliferative activities in a glioma model.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 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.
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.
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Who cites it
15 citing papers in PubMed.
- Distinct Responses of Estrogen Receptor α and β in Chondrocytes Under Excessive Mechanical Stress.Cartilage · 2026Article
- Estrogen α and β Receptor Expression in the Various Regions of Resected Glioblastoma Multiforme Tumors and in an In Vitro Model.International journal of molecular sciences · 2024Article
- Isoliquiritigenin as a modulator of the Nrf2 signaling pathway: potential therapeutic implications.Frontiers in pharmacology · 2024Review
- Substitutional Diversity-Oriented Synthesis and In Vitro Anticancer Activity of Framework-Integrated Estradiol-Benzisoxazole Chimeras.Molecules (Basel, Switzerland) · 2022Article
- The Impact of Estrogens and Their Receptors on Immunity and Inflammation during Infection.Cancers · 2022Review
- Estrogen Receptors as Molecular Targets of Endocrine Therapy for Glioblastoma.International journal of molecular sciences · 2021Review
- Insights into the role of estrogens and androgens in glial tumorigenesis.Journal of carcinogenesis · 2021Review
- Phytochemical and Pharmacological Role of Liquiritigenin and Isoliquiritigenin From Radix Glycyrrhizae in Human Health and Disease Models.Frontiers in aging neuroscience · 2018Review
- Estrogen nuclear receptors affect cell migration by altering sublocalization of AQP2 in glioma cell lines.Cell death discovery · 2018Article
- Update on the therapeutic significance of estrogen receptor beta in malignant gliomas.Oncotarget · 2017Review
- Estrogen receptor β, a regulator of androgen receptor signaling in the mouse ventral prostate.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Cyclic Ketoximes as Estrogen Receptor β Selective Agonists.ChemMedChem · 2016Article
- Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma.Scientific reports · 2016Article
- Prediction of selective estrogen receptor beta agonist using open data and machine learning approach.Drug design, development and therapy · 2016Article
- Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells.ChemMedChem · 2015Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
Estrogen receptor β (ERβ) selective agonists are considered potential therapeutic agents for a variety of pathological conditions, including several types of cancer. Their development is particularly challenging, since differences in the ligand binding cavities of the two ER subtypes α and β are minimal. We have carried out a rational design of new salicylketoxime derivatives which display unprecedentedly high levels of ERβ selectivity for this class of compounds, both in binding affinity and in cell-based functional assays. An endogenous gene expression assay was used to further characterize the pharmacological action of these compounds. Finally, these ERβ-selective agonists were found to inhibit proliferation of a glioma cell line in vitro. Most importantly, one of these compounds also proved to be active in an in vivo xenograft model of human glioma, thus demonstrating the high potential of this type of compounds against this devastating disease.
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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.