Binding of progestagens to receptor proteins in MCF-7 cells

作者: E.W. Bergink , F. van Meel , E.W. Turpijn , J. van der Vies

DOI: 10.1016/0022-4731(83)90371-0

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摘要: Abstract With the aim of finding an explanation for biological properties progestagens currently used contraceptive purposes, we have assessed their specificity progesterone, androgen and oestrogen receptors in MCF-7 cells. The progesterone cytosol fraction cells was similar to that human rabbit myometrial but different from receptor rat cytosol. At 37°C relative affinity 3-keto-desogestrel, major metabolite desogestrel, intact twice levonorgestrel Org 2058, three times medroxy-progesterone acetate (MPA), 4.5 norethisterone 5 cyproterone whereas at 4°C exposed molybdate (nontransformed complexes) 3-keto-desogestrel 2058 displayed affinity. stronger binding due higher stability its complex with receptor. half levonorgestrel. medroxyprogesterone (MPA) least than anti-androgenic activity there no clear difference between affinities androgenic anti-androgcnic properties. Of tested this study, only norethinodrel measurable very low We conclude present results studies correlate better known hormonal those obtained 4°C.

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