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Antiprogestins for breast cancer treatment: We are almost ready.
J Steroid Biochem Mol Biol
July 2024
Laboratory of Hormonal Carcinogenesis, Instituto de Biología y Medicina Experimental (IBYME CONICET), Buenos Aires, Argentina. Electronic address:
The development of antiprogestins was initially a gynecological purpose. However, since mifepristone was developed, its application for breast cancer treatment was immediately proposed. Later, new compounds with lower antiglucocorticoid and antiandrogenic effects were developed to be applied to different pathologies, including breast cancer.
View Article and Find Full Text PDFNext 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 PDFPersisting neuropsychiatric symptoms, Alzheimer's disease, and cerebrospinal fluid cortisol and dehydroepiandrosterone sulfate.
Alzheimers Res Ther
December 2022
Old Age Psychiatry, Department of Psychiatry, University Hospital of Lausanne, Lausanne, Switzerland.
Introduction: Neuropsychiatric symptoms are important treatment targets in the management of dementia and can be present at very early clinical stages of neurodegenerative diseases. Increased cortisol has been reported in Alzheimer's disease (AD) and has been associated with faster cognitive decline. Elevated cortisol output has been observed in relation to perceived stress, depression, and anxiety.
View Article and Find Full Text PDFClinical Utility of Mifepristone: Apprising the Expanding Horizons.
Cureus
August 2022
Department of Obstetrics and Gynecology, Pandit Deendayal Upadhyay Medical College, Rajkot, IND.
Mifepristone is a progesterone and glucocorticoid receptor antagonist. Medical abortion with mifepristone and prostaglandin has revolutionized the abortion process extending abortion care to the doors of females. From as low as 2 mg/day to doses extending to 600 mg, from daily dosing to single dosage treatment, mifepristone has a wide perspective in the treatment of various pathologies.
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