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Next step in the development of mesoprogestins: the preclinical profile of EC313.
Front Endocrinol (Lausanne)
September 2023
Evestra, Inc., Corporate Headquarters, Schertz, TX, United States.
Article Synopsis
- EC313 is a novel Selective Progesterone Receptor Modulator (SPRM) that exhibits both agonistic and antagonistic properties on the nuclear progesterone receptor, showing potential advantages over existing treatments.
- The estrogen-primed juvenile rabbit endometrium assay demonstrates that EC313 has stronger PR-agonistic effects than other mesoprogestins like Asoprisnil, indicating its effectiveness for conditions like uterine fibroids and endometriosis.
- In preclinical studies, EC313 effectively inhibits estrogenic activity and demonstrates superior anti-ovulatory effects without inducing premature labor, making it a promising candidate for further development in reproductive health treatments.
In vitro, in vivo, and in silico evaluation of the glucocorticoid receptor antagonist activity of 3,6-dibromocarbazole.
Food Chem Toxicol
October 2023
College of Food Science and Engineering, Jilin University, Changchun, 130062, China. Electronic address:
3,6-Dibromocarbazole is a novel environmental contaminant which is currently detected in several environmental media worldwide. This work aims to investigate the anti-glucocorticoid potency and endocrine disrupting effects of 3,6-dibromocarbazole. In vitro experiments indicated that 3,6-dibromocarbazole possessed glucocorticoid receptor (GR) antagonistic activity and inhibited dexamethasone-induced GR nuclear translocation.
View Article and Find Full Text PDFThe metastatic capacity of high-grade serous ovarian cancer cells changes along disease progression: inhibition by mifepristone.
Cancer Cell Int
December 2022
Experimental Pathology Unit, Department of Pathology, Faculty of Medicine and Health Sciences, McGill University, Montreal, QC, Canada.
Article Synopsis
- - The study compares traditional 2D assays with 3D organotypic models to assess the metastatic abilities of high-grade serous ovarian cancer cells, emphasizing that 3D models better mimic the in vivo environment seen in patients.
- - Using cancer cells from two patients at different disease stages, researchers found that while 2D assays showed decreasing migration and invasion rates with disease progression, late-stage cancer cells had a stronger adhesion to the 3D model.
- - Mifepristone, a drug tested in the study, was applied to evaluate its effect on cancer cell behavior, showing that late-stage disease cells could adhere more effectively, which correlates with their tumor capacity in actual patients.
Mifepristone Directly Disrupts Mouse Embryonic Development in Terms of Cellular Proliferation and Maturation In Vitro.
Toxics
November 2021
Department of Obstetrics and Gynecology, Kaohsiung Chang Gung Memorial Hospital, Chang Gung University College of Medicine, Kaohsiung 833, Taiwan.
Mifepristone (RU-486), a synthetic steroid with potent antiprogestogen and anti-glucocorticoid properties, has been widely used in clinical practice. Its effect on the endometrium, ovary, and fallopian tube has been well reported in many human and animal studies. However, its direct impact on post-implantation embryos remains underexplored.
View Article and Find Full Text PDFSelective Progesterone Receptor Modulators-Mechanisms and Therapeutic Utility.
Endocr Rev
October 2020
Department of Gynecology and Obstetrics, Division of Reproductive Sciences & Women's Health Research, Johns Hopkins Medicine, Baltimore, Maryland.
Selective progesterone receptor modulators (SPRMs) are a new class of compounds developed to target the progesterone receptor (PR) with a mix of agonist and antagonist properties. These compounds have been introduced for the treatment of several gynecological conditions based on the critical role of progesterone in reproduction and reproductive tissues. In patients with uterine fibroids, mifepristone and ulipristal acetate have consistently demonstrated efficacy, and vilaprisan is currently under investigation, while studies of asoprisnil and telapristone were halted for safety concerns.
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