The regulation of androgen-receptor turnover in human genital skin fibroblasts by 5α-dihydrotestosterone

1984 ◽  
Vol 12 (4) ◽  
pp. 658-659 ◽  
Author(s):  
DOROTHY RING ◽  
MALCOLM B. HODGINS
Keyword(s):  
Androgen Receptor ◽  
Skin Fibroblasts ◽  
Receptor Turnover

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

Androgen receptor isoforms AR-A and AR-B display functional differences in cultured human bone cells and genital skin fibroblasts

Steroids ◽  
2003 ◽  
Vol 68 (14) ◽  
pp. 1179-1187 ◽  
Author(s):  
Ute M. Liegibel ◽  
Ulrike Sommer ◽  
Irma Boercsoek ◽  
Ulrike Hilscher ◽  
Angelika Bierhaus ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Bone Cells ◽  
Skin Fibroblasts ◽  
Human Bone ◽  
Functional Differences ◽  
Receptor Isoforms

Regulation of the androgen receptor in human genital skin fibroblasts, with a review of sex steroid receptor regulation by homologous and heterologous steroids

1983 ◽  
Vol 61 (7) ◽  
pp. 770-778 ◽  
Author(s):  
Leonard Pinsky ◽  
Morris Kaufman ◽  
Carmen Gil-Esteban ◽  
Datevik Sumbulian
Keyword(s):  
Androgen Receptor ◽  
Calf Serum ◽  
Steroid Receptor ◽  
Skin Fibroblasts ◽  
Sex Steroid ◽  
Receptor Regulation ◽  
Time Pattern ◽  
Regulatory Behavior ◽  
Androgen Receptor Activity ◽  
Interexperimental Variation

When normal human genital skin fibroblasts are cultured for 3 days with 2–3 nM methyltrienolone (R1881, a synthetic nonmetabolizable androgen), they augment their specific androgen-receptor activity (two- to four-fold) with a time pattern that is always most rapid in the first 24 h, usually peaks by 48 h, and often declines, sometimes substantially, in the third 24-h interval. The time pattern is highly reproducible within experiments on confluent monolayers and is not influenced by the presence or absence of 10% fetal calf serum in the medium, the temperature (37 vs. 40 °C) at which the incubation is conducted, or the basal activity (up to 40 fmol/mg protein) that is saturated by incubation for 30–45 min at 37 °C. It does appear to be influenced by an unusually rapid increase in the first 24 h and by nonconfluent density of the monolayers, but these factors do not explain the considerable interexperimental variation, within and among cell lines, under nominally identical conditions. The time pattern is interpreted to represent an initial phase of "up-regulation" that is followed by one of compensatory adjustment, despite a constant level of unmetabolized ligand. A review of sex steroid receptor regulation by homologous and heterologous sex steroids reveals numerous examples of apparently homologous regulatory behavior.

Binding of androgens in 5α-reductase-deficient human genital skin fibroblasts: inhibition by progesterone and its metabolites

1982 ◽  
Vol 94 (3) ◽  
pp. 415-427 ◽  
Author(s):  
M. B. Hodgins
Keyword(s):  
Androgen Receptor ◽  
Androgen Receptors ◽  
Cultured Cells ◽  
Reductase Activity ◽  
External Genitalia ◽  
Skin Fibroblasts ◽  
Urogenital Sinus ◽  
Receptor Complexes ◽  
High Affinity ◽  
Receptor Sites

Binding of [3H]testosterone and 5α-dihydro[3H]testosterone ([3H]DHT) to specific androgen-receptor sites of 5α-reductase-deficient human genital skin fibroblasts (five cell-lines) was studied in the intact cultured cells at 37 °C. Under the conditions of the experiments, conversion of [3H]testosterone into [3H]DHT was negligible. Both steroids bound to the same set of high-affinity saturable sites in cytoplasmic and nuclear fractions of the cells. Unlabelled testosterone, DHT and methyltrienolone competed effectively with the labelled steroids. Progesterone and oestradiol were weaker competitors; cortisol did not compete. The dissociation constant (Kd) for high-affinity complexes with [3H]testosterone (0·44 ± 0·035 nmol/l) was higher than that for [3H]DHT complexes (0·20 ± 0·090 nmol/l). Unlabelled DHT was more effective than unlabelled testosterone in competing with either radioactive steroid. Complexes of [3H]DHT and receptor dissociated more slowly than [3H]testosterone-receptor complexes and [3H]DHT bound more extensively to low-affinity non-saturable sites in fibroblasts. As judged by competition with the radioactive androgens, progesterone bound to the androgen receptor with a Kd of about 7 nmol/l. 5α-Pregnane-3,20-dione had an approximately fivefold lower affinity than progesterone for androgen receptors; 3α/β- or 20α-reduction lowered its affinity further. It is suggested that in 5α-reductase deficiency in man, progesterone in amniotic fluid and blood could effectively inhibit testosterone binding to androgen receptors in the male embryonic external genitalia. One function of the high levels of 5α-reductase activity normally found in embryonic external genitalia and urogenital sinus may be to protect these tissues from the potentially antiandrogenic action of progesterone.

ANDROGEN RECEPTOR CHARACTERISTICS IN SKIN FIBROBLASTS FROM MEN WITH PUBERTAL MACROMASTIA

1983 ◽  
Vol 19 (2) ◽  
pp. 223-230 ◽  
Author(s):  
C. EIL ◽  
M. E. LIPPMAN ◽  
E. V. DE MOSS ◽  
D. LYNN LORIAUX
Keyword(s):  
Androgen Receptor ◽  
Skin Fibroblasts
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