Novel Mechanisms of Progesterone Antagonists and Progesterone Receptor

@article{Edwards2000NovelMO,
  title={Novel Mechanisms of Progesterone Antagonists and Progesterone Receptor},
  author={Dean P. Edwards and Susan A. Leonhardt and Elizabeth K. Gass-Handel},
  journal={Journal of the Society for Gynecologic Investigation},
  year={2000},
  volume={7},
  pages={S22 - S24}
}
The progesterone receptor (PR), as a member of the nuclear receptor superfamily of ligand-dependent transcription factors, activates gene transcription through binding to specific palindromic progesterone response elements (PRE) in the promoter region of progestin-responsive genes. The progesterone antagonists ZK98299 (Onapristone) and RU 486 (Mifepristone) inhibit the transcriptional activity of PR by complex mechanisms at concentrations much lower than the progestins. Altered conformation is… 
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Progesterone receptor transcription and non-transcription signaling mechanisms
Mechanism of Action of Progesterone Antagonists
TLDR
The first clinically used progesterone antagonist RU486 and closely related compounds are discussed and cellular factors that may influence the activity of these compounds, such as the availability of coactivators and corepressors and the context of specific target promoters in any given cell type are discussed.
Determination of conformational changes in the progesterone receptor using ELISA-like assays
Signal Transducer and Activator of Transcription 3 Is Expressed in the Decidualized Mesometrium of Pregnancy and Associates with the Progesterone Receptor Through Protein-Protein Interactions1
TLDR
Observations suggest thatSTAT3 expression is a prevalent feature of progesterone action, and that STAT3 and PR interactions represent a convergence of diverse signal transduction pathways in the decidualized mesometrium during pregnancy.
Dominant Role of Nuclear Progesterone Receptor in the Control of Rat Periovulatory Granulosa Cell Apoptosis1
TLDR
It is shown that P4 regulates apoptosis in periovulatory granulosa cells by acting via the classic nuclear receptor.
Inhibition of prostaglandin F2α synthesis and oxytocin receptor by progesterone antagonists in bovine endometrial cells in vitro
Differential expression of uterine calcium transporter 1 and plasma membrane Ca2+ ATPase 1b during rat estrous cycle.
TLDR
Results suggest that CaT1 is regulated by P4 at diestrus via a PR-dependent pathway, andCaT1 mRNA was expressed in uterine endometrium and glandularEndometrium atdiestrus in P4-treated rats.
Steroid Hormone Modulation of Prostaglandin Secretion in the Ruminant Endometrium During the Estrous Cycle1
  • A. Goff
  • Biology
    Biology of reproduction
  • 2004
TLDR
The purpose of this article is to review the recent data related to how progesterone and estradiol could regulate (initiate and then turn off) the uterine pulsatile secretion of PGF2α observed at luteolysis.
Comparative transcriptome profiling and characterization of gene expression for ovarian differentiation under RU486 treatment.
Progestins and antiprogestins affect gene expression in early development in zebrafish (Danio rerio) at environmental concentrations.
TLDR
Effects on the hormone system are elucidated by quantitative determination of transcriptional changes of target genes induced by 2, 20, and 200 ng/L P4, RU486, norethindrone (NET), and levonorgestrel (LNG).
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