PMID: 3762019Aug 15, 1986Paper

Inhibition of androgen receptor binding by natural and synthetic steroids in cultured human genital skin fibroblasts

Klinische Wochenschrift
M BreinerH U Schweikert

Abstract

The ability of various natural and synthetic steroids (some of which are widely used in clinical practice) to compete with dihydrotestosterone receptor binding in human genital skin fibroblasts was studied. Binding was assessed in fibroblast monolayers after incubation for 1 h at 37 degrees C with 2 nM 3H-dihydrotestosterone in the presence or absence of increasing concentrations of the steroid to be tested. Inhibition constants (Ki) were determined as the concentration of competitor-required for 50% inhibition of 3H-dihydrotestosterone binding. In addition, relative binding activity (RBA) of each test compound was calculated. Each competitor was tested in at least two different cell strains. The concentrations of unlabeled methyltrienolone (a synthetic nonmetabolizable androgen) and dihydrotestosterone for 50% inhibition of 3H-dihydrotestosterone binding were in the same order of magnitude, namely, 2 nM (2.2 respectively, 2.4 nM), whereas the affinity of testosterone was approximately one-fifth that of dihydrotestosterone. Other potent competitors for dihydrotestosterone binding were three progestins (norgestrel, gestoden, and medroxyprogesterone acetate) which have Ki values similar to testosterone. An order of magnitude lowe...Continue Reading

References

Nov 1, 1979·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·H U Schweikert
Jul 1, 1975·Endocrinology·P CorvolJ Mahoudeau
Oct 1, 1976·The Journal of Clinical Endocrinology and Metabolism·H U SchweikertJ D Wilson
Jan 1, 1983·The Journal of Clinical Endocrinology and Metabolism·D M WilbertJ D Wilson
Jul 1, 1984·The Journal of Clinical Endocrinology and Metabolism·C Eil, S K Edelson
Feb 1, 1981·The Journal of Clinical Endocrinology and Metabolism·I MowszowiczP Mauvais-Jarvis
Jan 24, 1980·The New England Journal of Medicine·J E Griffin, J D Wilson
Apr 13, 1981·Molecular and Cellular Biochemistry·T R Brown, C J Migeon
Sep 1, 1980·The Journal of Clinical Endocrinology and Metabolism·G Shapiro, S Evron

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Citations

Mar 4, 2000·International Journal of Urology : Official Journal of the Japanese Urological Association·N YanagisawaT Iwamoto
Jan 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·W D TilleyM J McPhaul
Jul 1, 1995·Clinical Endocrinology·H U SchweikertG Romalo
Jan 1, 1993·European Journal of Pediatrics·H U Schweikert
Sep 29, 2011·Molecular and Cellular Endocrinology·Nicole L MooreWayne D Tilley
Jan 23, 2015·Environmental Science & Technology·Vimal KumarHana Kocour Kroupová
Sep 10, 2003·Chembiochem : a European Journal of Chemical Biology·Smita S Muddana, Blake R Peterson
Aug 10, 2018·Toxicology Research·Ecem ÖzdemirMehmet Alper Çetinkaya
May 14, 1999·The Journal of Clinical Endocrinology and Metabolism·B ThieleK D Spindler
Apr 4, 2009·Journal of Chromatography. a·T F H Bovee, M G Pikkemaat

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