Presence of oestrogen receptors on target cells and antiproliferative activity of estramustine phosphate: Positive correlation for human tumours in vitro

Pavelić, Jasminka; Zgradić, I.; Pavelić, Krešimir

doi:10.1007/bf01625432

Cited by 7 publications

(1 citation statement)

References 22 publications

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“…Par ailleurs, alors que son effet estrogénique ne repré-sente que 1 % de celui de l'estradiol, l'effet de ce dernier sur l'inhibition de la tumeur est de quatre fois plus important, suggérant ainsi un mécanisme additionnel de l'EM. Sur des cultures de cellules tumorales humaines (rein, sein, prostate et utérus), l'EM a montré un effet d'inhibition de la prolifération cellulaire corrélée à la concentration des récepteurs aux estrogènes (RE) [18]. Dans une autre étude [8] sur cellules humaines de tumeur du sein issues de biopsies chez 306 patientes, il est apparu que 24 % des échantillons portaient des sites de fixation pour l'EM (EMBP) et ce taux était corrélé de façon significative avec l'absence ou le faible taux de récepteurs hormonaux.…”

Section: Toléranceunclassified

Estramustine: what is its place in 2010 in metastatic breast cancer?

Luporsi¹,

Guastalla²,

Médioni³

et al. 2010

Oncologie

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Estramustine: what is its place in 2010 in metastatic breast cancer?Abstract: Management of breast cancer remains difficult, especially in the metastatic phase. Estramustine may represent an additional therapeutic option, due to an appropriate mechanism of action and significant results in phase II trials: an objective response was obtained in 17.5-47% of cases, with estramustine alone or in combination with docetaxel in advanced metastatic cancers. In addition, estramustine is administered orally and its cost is low. Further studies are mandatory to assess this drug in association with targeted therapies and optimize the benefit/risk ratio, in defining the best prophylactic strategy to decrease the incidence of thrombotic events.Résumé : Le cancer du sein continue à poser des problèmes de prise en charge, notamment au stade métastatique. L'estramustine (EM) fait partie des molécules qui peuvent élargir la gamme des options thérapeutiques, en raison d'un rationnel pharmacologique pertinent et de résultats encourageants obtenus au cours d'études de phase II, en monothérapie ou en association au docétaxel, dans des cancers métastatiques (taux de ré-ponse objective compris entre 17,5 et 47 %). De plus, cette molécule a l'avantage d'être administrée par voie orale, avec un coût faible. Des études sont nécessaires pour évaluer l'EM en association aux thérapies ciblées et optimiser le rapport bénéfice/risque en définissant la meilleure stratégie de prévention des accidents thromboemboliques.

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Section: Toléranceunclassified

Estramustine: what is its place in 2010 in metastatic breast cancer?

Luporsi¹,

Guastalla²,

Médioni³

et al. 2010

Oncologie

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Interaction of bis-β-chlorethylamine estrogen derivatives with human ovarian adenocarcinoma cells

1999

Bull Exp Biol Med

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Antiproliferative effect of bis-~-chlorethylamine estrogen derivatives on human ovarian adenocarcinoma CaOV cells depends on the dose of the drug. In concentrations of 10 -5 and 5x10 -6 Mthey inhibit, while in a dose of 5x10 -7 M stimulate cell proliferation. It is assumed that CaOV cells express estradiol receptors. The interaction of these cytostatics with estrogenbinding sites on CaOV cells is demonstrated.

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Effects of synthetic bis-β-chloroethylamine estrogen derivatives on proliferation of skin sarcoma cells

et al. 2000

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The effects of four new synthetic bis-beta-chloroethylamine-containing estrogens and known cytostatic agents chlorophenacyl and estradiol mustard were compared on monolayer cultures of transformed L-929 fibroblasts (from murine skin sarcoma). The drugs within the concentration range of 10(-5)-5 10(-7)M inhibited proliferation of cultured cells by 67%. Chlorophenacyl displayed the least antiproliferative activity (15% inhibition at 10(-5) M). Steroid nucleus introduced into the molecule enhanced antiproliferative activity of test drug in comparison with chlorophenacyl, probably due to accumulation of the hormone-cytostatic molecules in cells. Estradiol had no effect on proliferative activity of L-929 cells, and no specific estrogen-binding sites were found in cultured transformed fibroblasts. The antiproliferative effect of hormone-cytostatics on this culture is not mediated via specific interactions with estrogen receptors.

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Presence of oestrogen receptors on target cells and antiproliferative activity of estramustine phosphate: Positive correlation for human tumours in vitro

Cited by 7 publications

References 22 publications

Estramustine: what is its place in 2010 in metastatic breast cancer?

Estramustine: what is its place in 2010 in metastatic breast cancer?

Interaction of bis-β-chlorethylamine estrogen derivatives with human ovarian adenocarcinoma cells

Effects of synthetic bis-β-chloroethylamine estrogen derivatives on proliferation of skin sarcoma cells

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