Characterization of estrogen-induced progestin binding in cytosol of the R3327 prostatic carcinoma of the rat.
High affinity binding of the synthetic steroids methyltrienolone (R1881) and promegestone (R5020) to cytosol protein from the Dunning (R3327) experimental prostatic carcinoma of the rat was investigated. Animals bearing tumours of approx 1.5 cm mean diameter were either left untreated, or were administered diethylstilbestrol diphosphate (DESP) in the drinking water in doses close to those used clinically for the treatment of human prostatic carcinoma. Tumours were excised after 10-40 days, and binding of [3H]R1881 and [3H]R5020 to tumour cytosol was characterized using Scatchard analysis, sucrose density gradient centrifugation, and steroid competition, under conditions optimal for the conservation and assay of progesterone receptor. Both ligands were bound in much higher concentrations by cytosol from DESP-treated tumours than from untreated tumours. Binding was of high affinity (Kd congruent to 1 nM), was specific for progestins, and sedimented in peaks at approximately 8S and approximately 4S in sucrose density gradients. We conclude the DESP treatment of rats bearing the R3327 prostatic carcinoma induces synthesis of progesterone receptor in this tumour.
D000230:Adenocarcinoma / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D002499:Centrifugation, Density Gradient; D003600:Cytosol / Q000378:metabolism; D004054:Diethylstilbestrol / Q000031:analogs & derivatives* / Q000494:pharmacology; D004963:Estrenes / Q000378:metabolism*; D008297:Male; D015741:Metribolone; D009649:Norpregnadienes / Q000378:metabolism*; D011397:Promegestone / Q000378:metabolism*; D011471:Prostatic Neoplasms / Q000378:metabolism*; D051381:Rats; D011980:Receptors, Progesterone / Q000378:metabolism
D004963:Estrenes; D009649:Norpregnadienes; D011980:Receptors, Progesterone; D015741:Metribolone; D004054:Diethylstilbestrol; D011397:Promegestone; C004955:fosfestrol