Obstruction of Estrogen-Receptor Complex Formation. Further Analysis of the Nature and Steroidal Specificity of the Effect12
| Autor: | Gary H. Watson, Thomas G. Muldoon, Kenneth S. Korach |
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| Rok vydání: | 1977 |
| Předmět: | |
| Zdroj: | Endocrinology. 101:1733-1743 |
| ISSN: | 1945-7170 0013-7227 |
| DOI: | 10.1210/endo-101-6-1733 |
| Popis: | Qualitative and quantitative aspects of inhibition of 17β-estradiol-receptor complex formation by a number of natural and synthetic hormonal agents have been investigated in rat anterior pituitary cytosol. The initial velocity of the interaction between 17β-estradiol and its receptors is impeded by preincubation with androgenic compounds in a dose-related manner, the order of inhibitory effectiveness being: 3β-androstanediol > 3α-androstanediol = 5α-dihydrotestosterone > testosterone. Equivalence of 3α-androstanediol and 5α-dihydrotestosterone effectiveness can be accounted for by high cytoplasmic activity of 3α-hydroxysteroid dehydrogenase. Both initial velocity and inhibitory response to a given level of androgen are lower in the male than in female cytosol; the variation appears to be the consequence of different endogenous androgen levels. Weak androgens (dehydroepiandrosterone and etiocholanolone) and anti-androgens (flutamide, cyproterone and Ro7-8117) are effective inhibitors, but the degree of inh... |
| Databáze: | OpenAIRE |
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