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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.
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The role of progesterone and the progesterone receptor in cancer

Expert Review of Endocrinology & Metabolism, 2017
There is an abundance of accumulating data strongly suggesting there is a key role for the progesterone receptor in the molecular events effecting the growth or containment of a variety of cancers. This knowledge should lead to novel new strategies to combat various cancers, including drugs classified as progesterone receptor modulators or monoclonal ...
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UTERINE PROGESTERONE AFTER PROGESTERONE TREATMENT: ON THE DISAPPEARANCE OF CYTOSOLIC PROGESTERONE RECEPTORS

Journal of Steroid Biochemistry, 1979
Abstract The effect of progesterone (P) treatment on P receptors and on the resultant P concentrations in the cytoplasm and other subcellular fractions was studied. Cytoplasmic P receptors in the uterus of oestrogenized rabbits were reduced by about 60% after 24 h of single injection of P.
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Receptors for progesterone

Gynecologic Oncology, 1974
Abstract Coordinated estrogen- and progesterone-induced changes regulate biological functions of the endometrium. The uterine deciduoma reaction is used as a model in defining the mechanism of the progesterone-induced endometrial transformations. Uterine progesterone concentrations were determined by radioimmunoassay during three critical periods ...
B R, Rao, W G, Wiest
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A radioimmunoassay for progesterone

Steroids, 1972
Abstract The need for a simple and fast quantitative method for progesterone with routine laboratory and clinical application motivated the development of a radioimmunoassay. Progesterone antibodies were produced in rabbits by immunization with a bovine serum albumin conjugate of 11α-hydroxyprogesterone hemisuccinate.
J M, Spieler   +3 more
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Progesterone and ovulation

European Journal of Obstetrics & Gynecology and Reproductive Biology, 2001
The role of progesterone (P) in the mechanism of ovulation is controversial at best. The contraceptive application of P was established in rodents in 1936 and with orally absorbed progestogenes was put to human use. There were hints on the proovulatory actions of P administered before the time of ovulation in rats by 1948.
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Progesterone and pregnancy

Current Opinion in Obstetrics & Gynecology, 2005
Progesterone is an essential hormone in the process of reproduction. Although the pharmacokinetics and pharmacodynamics of progesterone have been well studied, its use in the pathophysiology of pregnancy remains controversial. One of these concerns is the way in which the hormone is administered.In obstetrics the most frequent uses of progesterone are ...
Gian Carlo, Di Renzo   +3 more
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The Case for Progesterone

Annals of the New York Academy of Sciences, 2005
Abstract: Recent clinical trials in hormone therapy (HT) for women approaching or past menopause have been disappointing. Most women who have been taking conjugated equine estrogens combined with synthetic progestins have been encouraged to stop these supplements because of increased health risks.
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Spinimmunoassay of progesterone

Biochemical and Biophysical Research Communications, 1975
Abstract A spin-labeled derivative of progesterone was prepared: 3(progesterone-1111α-hemisuccinyl)-3 methylamino-2,2,5,5, tetramethyl pyrolidine-1-oxyl. A corresponding antibody was produced by inoculating rabbits with progesterone-11α-hemisuccinyl-(bovine serum albumin). These materials were then used in developing a method to measure progesterone.
R, Wei, R, Almirez
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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   +5 more
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