ArticleScientific reports2016
Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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Who cites it
48 citing papers in PubMed, 71 citations in OpenAlex.
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- Estrogen regulation in the prostate underlies racial disparity in men with benign prostatic hyperplasia.The Journal of pathology · 2026Article
- Estrogen receptor β stimulation as a possible novel therapeutic target for cutaneous T-cell lymphoma.Blood advances · 2025Article
- ERβ mediates sex-specific protection in the App-NL-G-F mouse model of Alzheimer's disease.Biology of sex differences · 2025Article
- An Estrogen Receptor β Agonist with AR Antagonist Activity from a Modern AsymmetricACS medicinal chemistry letters · 2025Article
- The Genistein Supply and Elemental Composition of Rat Kidneys in an Induced Breast Cancer Model.Nutrients · 2025Article
- Clinical development and informatics analysis of natural and semi-synthetic flavonoid drugs: A critical review.Journal of advanced research · 2024Review
- Estrogen Signals through ERβ in Breast Cancer; What We Have Learned since the Discovery of the Receptor.Receptors (Basel, Switzerland) · 2024Article
- A Review of Approaches to Potentiate the Activity of Temozolomide against Glioblastoma to Overcome Resistance.International journal of molecular sciences · 2024Review
- Preclinical Development of Brain Permeable ERβ Agonist for the Treatment of Glioblastoma.Molecular cancer therapeutics · 2023Article
- Review
- The radioprotectant nano-genistein enhances radiotherapy efficacy of lung tumors in mice.Translational lung cancer research · 2023Article
- Glioblastoma in pregnant patient with pathologic and exogenous sex hormone exposure and family history of high-grade glioma: A case report and review of the literature.Surgical neurology international · 2023Article
- Potentiation of temozolomide activity against glioblastoma cells by aromatase inhibitor letrozole.Cancer chemotherapy and pharmacology · 2022Article
- Targeting Several Biologically Reported Targets of Glioblastoma Multiforme by Assaying 2D and 3D Cultured Cells.Cellular and molecular neurobiology · 2022Article
- Hormonal Crosstalk Between Thyroid and Breast Cancer.Endocrinology · 2022Review
- Therapeutic Targeting of Ovarian Cancer Stem Cells Using Estrogen Receptor Beta Agonist.International journal of molecular sciences · 2022Article
- Our evolving understanding of how 27-hydroxycholesterol influences cancer.Biochemical pharmacology · 2022Review
- Different Susceptibilities of Human Melanoma Cell Lines to G2/M Blockage and Cell Death Activation in Response to the Estrogen Receptor β agonist LY500307.Journal of Cancer · 2022Article
- KDM1A inhibition augments the efficacy of rapamycin for the treatment of endometrial cancer.Cancer letters · 2022Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
Abstract
Glioblastomas (GBM), deadly brain tumors, have greater incidence in males than females. Epidemiological evidence supports a tumor suppressive role of estrogen; however, estrogen as a potential therapy for GBM is limited due to safety concerns. Since GBM express ERβ, a second receptor for estrogen, targeting ERβ with a selective agonist may be a potential novel GBM therapy. In the present study, we examined the therapeutic effect of the selective synthetic ERβ agonist LY500307 using in vitro and in vivo GBM models. Treatment with LY500307 significantly reduced the proliferation of GBM cells with no activity on normal astrocytes in vitro. ERβ agonists promoted apoptosis of GBM cells, and mechanistic studies using RNA sequencing revealed that LY500307 modulated several pathways related to apoptosis, cell cycle, and DNA damage response. Further, LY500307 sensitized GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide. LY500307 treatment significantly reduced the in vivo tumor growth and promoted apoptosis of GBM tumors in an orthotopic model and improved the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model. Our results demonstrate that LY500307 has potential as a therapeutic agent for GBM.
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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.