The use of a hydroxylapatite-filter steroid receptor assay method in the study of the modulation of androgen receptor interaction |
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| Authors: | S Liao D Witte K Schilling C Chang |
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| Affiliation: | 1. Masonic Cancer Center, University of Minnesota, Minneapolis, MN, USA;2. Department of Medicine-Hematology, Oncology & Transplantation, University of Minnesota, Minneapolis, MN, USA;3. Department of Laboratory Medicine and Pathology, University of Minnesota, Minneapolis, MN, USA;4. Department of Urology, University of Minnesota, Minneapolis, MN, USA;1. Molecular Endocrinology Laboratory, Department of Cellular and Molecular Medicine, Campus Gasthuisberg ON1 Herestraat 49 - box 901, Leuven 3000, Belgium;2. Department of Chemistry, Laboratory of Biomolecular Modelling and Design, Heverlee 3001, Belgium;1. Department of Biochemistry and Functional Genomics, Université de Sherbrooke, Sherbrooke, QC, Canada;2. The Medical Physics Unit, McGill University Health Center, Montreal, QC, Canada |
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| Abstract: | Receptors for androgen, estrogen, and glucocorticoid can be assayed by hydroxylapatite adsorption of the radioactive steroid-receptor complex and washing of the adducts on membrane filters mounted on a multiple filter holder. The method is economical, very rapid and sensitive. This new receptor assay method was used to study the modulation of androgen receptor of rat ventral prostate by metal ions, thiols, and ligand structure. The interaction of androgen with the naked receptor is inhibited by 10 microM ZnCl2, CdSO4, or CuSO4 but this inhibition is competed by androgen and is reversed by DTT. The androgen-receptor complex is less sensitive to divalent metal ions but Zn2+, at 3 mM, appears to alter the conformation of the receptor and promote the release of androgen. Certain phenanthrene derivatives exhibited striking structural specificities in their ability to compete with radioactive androgen for binding to the prostate receptor. The results suggest that the receptor has binding preference toward individual ring structure in the steroid. |
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