Characterization of unoccupied (R) and occupied (RA) androgen binding components of the hyperplastic human prostate. |
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Authors: | S A Shain R W Boesel D L Lamm H M Radwin |
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Institution: | 1. Department of Cellular and Molecular Biology, Southwest Foundation for Research and Education USA;2. Audie Murphy Memorial Veterans Administration Hospital USA;3. Department of Surgery, University of Texas Health Science Center, San Antonio, TexasUSA |
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Abstract: | Saturation protocols were developed for measurement of unoccupied (R) and steroid-occupied (RA) androgen binding components of human hyperplastic prostate. The concentration of unoccupied cytoplasmic binding sites (2 hr incubation at 2 degrees C) for the synthetic androgen R1881 (17beta-hydroxy-17alpha-methyl-estra-4,9,11-trien-3-one) and the synthetic progestin R5020 (17alpha,21-dimethyl-19-norpregna-4,9-diene-3,20-dione) respectively was 10.7 +/- 1.4 and 14.3 +/- 3.2 fmoles per mg cytosol protein and the apparent steroid affinity respectively was 9.6 +/- 0.8 and 1.6 +/- 0.4 x 10(8) M-1. Steroid specificity of the unoccupied cytoplasmic R1881 and R5020 binding sites was similar. When R1881 and R5020 were employed as probes of total, R plus RA, cytoplasmic binding components (20-24 hr incubation at 15 degrees C) saturable binding of R5020 was not detectable. Total cytoplasmic R1881 binding site concentration and apparent affinity for R1881 were 51.7 +/- 3.3 fmoles per mg cytosol protein and 2.7 +/- 0.6 x 10(7) M-1. R5020 was a poor inhibitor of R1881 binding to total cytoplasmic R1881 binding components. |
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Keywords: | Cortisol: 11 β 17α 21-trihydroxy-4-pregnene-3 20-dione 17β-estradiol: 1 3 5(10)- estratriene-3 17β-diol 19-nortestosterone: 17β-hydroxy-4-estren-3-one Progesterone: 4-pregnene-3 20-dione 17α-testosterone epitestosterone: 17α-hydroxy-4-androsten-3-one 17β-testosterone: 17β-hydroxy-4-androsten-3-one |
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