Zinc potentiation of androgen receptor binding to nuclei in vitro

Biochemistry ◽  
1984 ◽  
Vol 23 (15) ◽  
pp. 3471-3478 ◽  
Author(s):  
Douglas S. Colvard ◽  
Elizabeth M. Wilson
Keyword(s):  
Androgen Receptor ◽  
Receptor Binding

In Vitro Androgen Receptor Binding Affinity and in Vivo Inhibitory Activity of 5?-Pregnane-3, 20-Dione

1988 ◽  
Vol 529 (1 Fourth Colloq) ◽  
pp. 239-241
Author(s):  
SAUDHAMINI PARTHASARATHY ◽  
ANDREA CHIN ◽  
VIRGINIA MALLOY ◽  
JONATHAN MATIAS
Keyword(s):  
Androgen Receptor ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Inhibitory Activity ◽  
Receptor Binding Affinity

Metabolism and receptor binding of nandrolone and testosterone under in vitro and in vivo conditions

1985 ◽  
Vol 110 (3_Suppla) ◽  
pp. S31-S37 ◽  
Author(s):  
E. W. Bergink ◽  
J. A. A. Geelen ◽  
E. W. Turpijn
Keyword(s):  
Androgen Receptor ◽  
Receptor Binding ◽  
Reductase Activity ◽  
Hydroxysteroid Dehydrogenase ◽  
In Vivo Studies ◽  
Muscular Tissue ◽  
Binding Studies ◽  
Tissue Homogenates

Abstract. The metabolism and receptor binding of nandrolone (N) and testosterone (T) were studied under in vitro and in vivo conditions. The results of both in vitro incubation studes with 3H-N and 3H-T in tissue homogenates from rats and in vivo infusion studies with 3H-N and 3H-T in conscious rats show the importance of the enzymes 5α-reductase and 3α/β-hydroxysteroid-oxidoreductases in the prostate and the importance of the enzyme 17β-hydroxysteroid dehydrogenase in the kidney for the effects of N and T on these tissues. Following infusion of a combined dose of 3H-N and 3H-T there is a preferential retention at the receptor of 5α-dihydrotestosterone (DHT) over 5α-dihydronandrolone (DHN), N and T (DHT ⪢ DHN > N > T) in the prostate because T is a better substrate than N for 5α-reductase and because DHT binds more strongly to the androgen receptor than DHN, N and T. In the kidney 5α-reductase is not important; there is a preferential retention of N in T (DHN and DHT were only present in small amounts) because N is less susceptible than T for metabolic inactivation by the enzyme 17β-hydroxysteroid dehydrogenase and N binds strongly to the androgen receptor. Both in vitro and in vivo studies show that N and T were relatively stable in spleen, thymus and muscular tissue (only shown in vivo) and, as a result, the same amount of N and T was bound to the receptor in these tissues in the in vivo infusion experiment. In vitro binding studies with the androgen receptor in intact human cells show that 5α-reduction increases the affinity of T and decreases the affinity of N and of the 17α-ethyl derivative of N (3-keto-ethylestrenol). The results of the present studies explain the relatively strong effect of N, or derivatives of N, compared to that of T on tissues devoid of 5α-reductase activity (e.g. muscular tissue) and they suggest that in particular there may be a strong effect of N on tissues which in addition have a high 17β-hydroxysteroid dehydrogenase activity (e.g. kidney).

scholarly journals Evaluation of OASIS QSAR Models Using ToxCast™ in Vitro Estrogen and Androgen Receptor Binding Data and Application in an Integrated Endocrine Screening Approach

2016 ◽  
Vol 124 (9) ◽  
pp. 1453-1461 ◽  
Author(s):  
Barun Bhhatarai ◽  
Daniel M. Wilson ◽  
Paul S. Price ◽  
Sue Marty ◽  
Amanda K. Parks ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Receptor Binding ◽  
Screening Approach ◽  
Binding Data ◽  
Qsar Models

Some aspects of androgen insensitivity

1986 ◽  
Vol 113 (4_Suppl) ◽  
pp. S386-S395 ◽  
Author(s):  
I.A. HUGHES ◽  
B.A.J. EVANS
Keyword(s):  
Androgen Receptor ◽  
Receptor Binding ◽  
Gene Locus ◽  
Specific Binding ◽  
Linked Gene ◽  
Androgen Insensitivity ◽  
Phenotypic Spectrum ◽  
Endocrine Features

Abstract. The clinical and endocrine features of the syndromes of androgen insensitivity which display a wide phenotypic spectrum are reviewed. A simple, dispersed whole cell assay to study androgen receptor binding in genital skin fibroblasts has been used to determine the pathogenesis of androgen insensitivity. Classification of the disorders based on in vitro studies does not show absolute concordance with the clinical sub-groups. Androgen-induced augmentation of basal specific binding is proposed as a possible functional test of androgen responsiveness in disorders such as partial androgen insensitivity, isolated hypospadias and micropenis. Understanding the cause of androgen insensitivity in many receptor-positive patients awaits identification and isolation of DNA probes for the X-linked gene locus for the androgen receptor.

Inhibition of androgen receptor binding by drugs in cultured human genital skin fibroblasts

1986 ◽  
Vol 113 (1_Suppl) ◽  
pp. S152
Author(s):  
M. BREINER ◽  
G. ROMALO ◽  
H.U. SCHWEIKERT
Keyword(s):  
Androgen Receptor ◽  
Receptor Binding ◽  
Skin Fibroblasts
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