ArticleMolecular cancer therapeutics2013
A second-generation 2-Methoxyestradiol prodrug is effective against Barrett's adenocarcinoma in a mouse xenograft model.
Article in Molecular cancer therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 28 citations in OpenAlex.
- [Gender medicine in diseases of the upper gastrointestinal tract].Chirurgie (Heidelberg, Germany) · 2024Review
- Inhibition of the HIF-1 Survival Pathway as a Strategy to Augment Photodynamic Therapy Efficacy.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Evidence for 2-Methoxyestradiol-Mediated Inhibition of Receptor Tyrosine Kinase RON in the Management of Prostate Cancer.International journal of molecular sciences · 2021Article
- 2-Methoxyestradiol improves the apoptosis level in keloid fibroblasts through caspase-dependent mechanismsAmerican journal of translational research · 2018Article
- G-1 Inhibits Breast Cancer Cell Growth via Targeting Colchicine-Binding Site of Tubulin to Interfere with Microtubule Assembly.Molecular cancer therapeutics · 2017Article
- Inhibition of proliferation and invasion in 2D and 3D models by 2-methoxyestradiol in human melanoma cells.Pharmacological research · 2017Article
- A novel intraperitoneal metastatic xenograft mouse model for survival outcome assessment of esophageal adenocarcinoma.PloS one · 2017Article
- Novel delivery approaches for cancer therapeutics.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Animal Models of Barrett's Esophagus and Esophageal Adenocarcinoma-Past, Present, and Future.Clinical and translational science · 2015Review
- Aspirin blocks growth of breast tumor cells and tumor-initiating cells and induces reprogramming factors of mesenchymal to epithelial transition.Laboratory investigation; a journal of technical methods and pathology · 2015Article
- Association between circulating levels of sex steroid hormones and Barrett's esophagus in men: a case-control analysis.Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association · 2015Article
- Article
- Pancreatic tumor cell secreted CCN1/Cyr61 promotes endothelial cell migration and aberrant neovascularization.Scientific reports · 2014Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
2-Methoxyestradiol (2-ME2) is an endogenous metabolite of estradiol. In preclinical models, 2-ME2 is effective against different types of tumors. Unfortunately, only low systemic concentrations of 2-ME2 can be achieved following oral administration, even after very high doses are administered to patients. In an effort to solve this problem, we have now synthesized and tested a new prodrug of 2-ME2 that is water-soluble due to a bioreversible hydrophilic group added at the 3-position and that more effectively resists metabolic inactivation due to an ester moiety added to mask the 17-position alcohol. We are reporting here for the first time that this double prodrug of 2-ME2 is effective as an antiproliferative and anticancer agent for both in vitro and in vivo studies against Barrett esophageal adenocarcinoma (BEAC) and provided greater potency than 2-ME2 in inhibiting the growth of BEAC xenografts. Finally, studies indicate that, like 2-ME2, the 2-ME2-PD1 exhibits anticancer effect through possible disruption of microtubule network.
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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.