Characterization and Measurement of the Androgen Receptor in Human Benign Prostatic Hyperplasia and Prostatic Carcinoma
| Autor: | Peter Ekman, Bertil Högberg, Jan-Ake Gustafsson, Åke Pousette, Dominique Bression, Marek Snochowski, Lennart Andersson |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
medicine.medical_specialty
Chemistry Endocrinology Diabetes and Metabolism Biochemistry (medical) Clinical Biochemistry Cyproterone acetate Hyperplasia medicine.disease Biochemistry Androgen receptor Prostate cancer chemistry.chemical_compound Endocrinology medicine.anatomical_structure Prostate Internal medicine medicine Cyproterone Estramustine Receptor medicine.drug |
| Zdroj: | The Journal of Clinical Endocrinology & Metabolism. 45:920-930 |
| ISSN: | 1945-7197 0021-972X |
| Popis: | [6,7-3H]Methyltrienolone (R 1881) has been used as ligand to measure and characterize the androgen receptor in human benign prostatic hyperplasia and prostatic carcinoma. [3H]R 1881 was bound with high affinity and low capacity to cytosol from six out of nine specimens of transvesically enucleated benign prostatic hyperplasia and from two specimens of prostate carcinoma obtained by Veenema biopsy or transvesical enucleation. The dissociation constant of the [3H]R 1881-receptor complex was in the range of 0.3–1.8 × 10−9M and the number of binding sites 9–26 fmoles/mg protein. [3H]R 1881 was displaced from its binding sites on the receptor by 5α-dihydrotestosterone and testosterone; much less efficient competitors were LS 1727, cyproterone acetate, 17β-estradiol, R 5020, 5α-androstane-3α,17β-diol and progesterone, whereas 4-androstene-3,17-dione, cyproterone, estramustine and cortisol did not compete. The receptor was stable at 0 C but was degraded rapidly (t½ = 14 min) at 37 C. The rate of dissociation of ... |
| Databáze: | OpenAIRE |
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