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Characterization of new estrogen receptor destabilizing compounds: effects on estrogen-sensitive and tamoxifen-resistant breast cancer.
Two new pure antiestrogens-ZK-703 and ZK-253-that belong to the class of specific estrogen receptor destabilizers (SERDs) that are more effective than tamoxifen or fulvestrant at inhibiting the growth of ER-positive breast cancer in all xenograft models are characterized. Expand
Progesterone antagonists: Tumor-inhibiting potential and mechanism of action
It is shown that the progesterone antagonists, Onapristone and ZK 112993, which possess a reduced antiglucocorticoid activity compared to Mifepristone, exert a strong tumor-inhibiting effect in a panel of hormone-dependent mammary tumor models. Expand
Progesterone receptor repression by estrogens in rat uterine epithelial cells
It is shown that in the rat the activated ER induces diverging effects on PR expression in different cell types even within the same organ, as in the cell types of the target organs uterus and breast. Expand
Antitumor activity of the antiprogestins ZK 98.299 and RU 38.486 in hormone dependent rat and mouse mammary tumors: Mechanistic studies
The results indicate that the main mechanism of the antitumor action of antiprogesterones in these models is a direct progesterone receptor-mediated antiproliferative effect at the level of the mammary tumor cells, most probably via the induction of terminal differentiation associated with terminal cell death. Expand
Pharmacokinetic and pharmacological features of oestradiol valerate.
Differences of practical significance exist in respect of the quantitative effect of oestradiol valerate following oral and intramuscular administration, whereas 4 mg oestrogens administered intramUScularly is therapeutically sufficient for a period of 2-4 wk (depot effect), as much as 2 mg daily over 3 wk must be administered via the oral route to achieve the same effect. Expand
Effects of partial versus pure antiestrogens on ovulation and the pituitary–Ovarian axis in the rat
  • J. Donath, Y. Nishino
  • Medicine, Biology
  • The Journal of Steroid Biochemistry and Molecular…
  • 1 August 1998
Comparisons of the effects of the pure antiestrogen ZM and the partial agonist tamoxifen on ovulation and peripheral hormone levels in the rat suggest that ZM inhibits not only the positive but also negative feedback effect of estrogens and TAM seems to inhibit only thepositive feedback. Expand
Potentiation of the antitumor effect of tamoxifen by combination with the antiprogestin onapristone
The findings suggest that the high antitumor effect of the combination of TAM and ON compared to the corresponding monotherapies can be related not only to the interaction of antihormones and receptors, but also to the up-regulation of PR and to a decrease in progesterone production. Expand
Estrogenic partial effect of norethisterone enanthate in relation to tumor induction in rat mammary gland.
The estrogenic partial effect of norethisterone enanthate seems to have no significance in humans, and the optimal dose ratio between estrogens and progesterone for maintenance of physiological functions of target organs is quite different from species to species. Expand
The prostate growth stimulation by progesterone is due to androgenic products and progesterone receptor-mediated mechanisms.
The localization of progesterone (P4) receptors (PR) in prostate and prostatic tumors is found and the involvement of P4 in the mechanism of hormone-dependent growth of prostate and tumors is suggested. Expand