Results 311 to 320 of about 157,138 (359)

Novel Mechanisms of Progesterone Antagonists and Progesterone Receptor

Journal of the Society for Gynecologic Investigation, 2000
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.
D P, Edwards, S A, Leonhardt, E, Gass-Handel   +2 more
openaire   +2 more sources

Progesterone receptor and the mechanism of action of progesterone antagonists

The Journal of Steroid Biochemistry and Molecular Biology, 1995
Currently available progesterone antagonists have been suggested to fall into two categories based on differences in how they interact with and inactivate the progesterone receptor (PR). The anti-progestin ZK98299 (Type I) impairs PR association with DNA, while Type II compounds (RU486, ZK112993, ZK98734) promote PR binding to DNA.
D P, Edwards, M, Altmann, A, DeMarzo, Y, Zhang, N L, Weigel, C A, Beck   +5 more
openaire   +2 more sources

Progesterone antagonists and progesterone receptor modulators

Expert Opinion on Investigational Drugs, 2003
Since the discovery of the antiprogestin RU 486 (mifepristone), other compounds have been synthesised that function as pure progesterone antagonists or progesterone receptor modulators. The latter are mixed agonists-antagonists. Mifepristone is usually used to terminate pregnancy but these compounds have numerous other applications in female healthcare.
openaire   +2 more sources

The evolution of progesterone receptor ligands

Medicinal Research Reviews, 2006
AbstractProgesterone is one of the first nuclear receptor hormones to be described functionally and subsequently approached as a drug target. Because progesterone (1) affects both menstruation and gestation via the progesterone receptor (PR), research aimed at modulating its activity is usually surrounded by controversy.
Kevin P, Madauss, Eugene L, Stewart, Shawn P, Williams   +2 more
openaire   +2 more sources

Progesterone-Progestin Receptors

1974
A correlation between binding to the progestin-specific uterine cytosol receptor and with well-defined facets of progesterone action was established. Structurally similar derivatives of norprogesterone and nortestosterone were compared. Binding was measured in vitro by determining their competitive effect on the progestin-tagged uterine cytosol ...
J P, Raynaud, D, Philibert, G, Azadian-Boulanger   +2 more
openaire   +2 more sources

Progesterone Receptors and Ovulation

2010
The steroid hormone, progesterone, plays a critical role in the regulation of female ovulation. The physiological effects of progesterone are mediated by two nuclear receptor transcription factors, PR-A and PR-B, which are produced from a single gene and upon binding progesterone regulate the expression of specific gene networks in reproductive tissues.
openaire   +2 more sources

Progesterone ”Receptor“ in Rat Ovary*

Endocrinology, 1979
A soluble thermolabile protein with many characteristics of a progesterone receptor has been identified in ovaries of estrogen-stimulated, hypophysectomized, immature female rats. A potent synthetic progestin R5020 (17,21-dimethyl-19-nor-pregna-4, 9-diene-3, 20-dione) and a progestin-receptor complex stabilizer (glycerol) were employed.
J R, Schreiber, J W, Hsueh
openaire   +2 more sources

Progesterone Receptor Signaling Mechanisms

Journal of Molecular Biology, 2016
Progesterone receptor (PR) is a master regulator in female reproductive tissues that controls developmental processes and proliferation and differentiation during the reproductive cycle and pregnancy. PR also plays a role in progression of endocrine-dependent breast cancer.
Sandra L, Grimm, Sean M, Hartig, Dean P, Edwards   +2 more
openaire   +2 more sources

Progesterone antagonists and progesterone receptor modulators: an overview

Steroids, 2003
Since the original description of the structure of the antiprogestin, mifepristone, was published, numerous related compounds have been synthesized which may function as progesterone antagonists (PAs) or progesterone receptor modulators (PRMs). The latter are mixed agonists-antagonists.
openaire   +2 more sources

Progesterone Receptors in Rat Thymus

Endocrinology, 1983
Tritiated promegestone ([3H]R5020) is bound with high affinity in cytosol prepared from the thymus gland of both male and female rats. To prevent tracer binding to glucocorticoid receptors, we have used excess RU26988 (11 beta, 17 beta-dihydroxy-21-methyl-17 alpha-pregna-1,4,6-trien-20-yn-3-one), a highly specific synthetic glucocorticoid.
P T, Pearce, B A, Khalid, J W, Funder
openaire   +2 more sources