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Binding of [3H]methyltrienolone to androgen receptor in rat liver.
Biochim Biophys Acta. 1984 Aug 21; 800(3):214-9.BB

Abstract

The synthetic androgen methyltrienolone is superior to testosterone and androstenedione for the measurement of androgen receptor in tissues where the native ligands are metabolized into inactive derivatives. [3H]Methyltrienolone binds with a high affinity to androgen receptor in cytosol prepared from male rat livers, as the Scatchard analysis revealed that the Kd value was 3.3 X 10(-8) M and the number of binding sites was 35.5 fmol/mg protein. Since methyltrienolone also binds glucocorticoid receptor which exists in rat liver, the apparent binding of androgen receptor is faulty when measured in the presence of glucocorticoid receptor. The binding of methyltrienolone to glucocorticoid receptor can be blocked by the presence of a 100-fold molar excess of unlabeled synthetic glucocorticoid, triamcinolone acetonide, without interfering in its binding to androgen receptor, because triamcinolone does not bind to androgen receptor. Triamcinolone-blocked cytosol exhibited that the Kd value was 2.5 X 10(-8) M and the number of binding sites was 26.3 fmol/mg protein, indicating a reduction to 3/4 of that in the untreated cytosol. The profile of glycerol gradient centrifugation indicated that [3H]methyltrienolone-bound receptor migrated in the 8-9 S region in both untreated and triamcinolone-blocked cytosols, but the 8-9 S peak in triamcinolone-blocked cytosol was reduced to about 3/4 of that of untreated cytosol.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

6331850

Citation

Kyakumoto, S, et al. "Binding of [3H]methyltrienolone to Androgen Receptor in Rat Liver." Biochimica Et Biophysica Acta, vol. 800, no. 3, 1984, pp. 214-9.
Kyakumoto S, Sato N, Nemoto T, et al. Binding of [3H]methyltrienolone to androgen receptor in rat liver. Biochim Biophys Acta. 1984;800(3):214-9.
Kyakumoto, S., Sato, N., Nemoto, T., Ohara-Nemoto, Y., & Ota, M. (1984). Binding of [3H]methyltrienolone to androgen receptor in rat liver. Biochimica Et Biophysica Acta, 800(3), 214-9.
Kyakumoto S, et al. Binding of [3H]methyltrienolone to Androgen Receptor in Rat Liver. Biochim Biophys Acta. 1984 Aug 21;800(3):214-9. PubMed PMID: 6331850.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Binding of [3H]methyltrienolone to androgen receptor in rat liver. AU - Kyakumoto,S, AU - Sato,N, AU - Nemoto,T, AU - Ohara-Nemoto,Y, AU - Ota,M, PY - 1984/8/21/pubmed PY - 1984/8/21/medline PY - 1984/8/21/entrez SP - 214 EP - 9 JF - Biochimica et biophysica acta JO - Biochim. Biophys. Acta VL - 800 IS - 3 N2 - The synthetic androgen methyltrienolone is superior to testosterone and androstenedione for the measurement of androgen receptor in tissues where the native ligands are metabolized into inactive derivatives. [3H]Methyltrienolone binds with a high affinity to androgen receptor in cytosol prepared from male rat livers, as the Scatchard analysis revealed that the Kd value was 3.3 X 10(-8) M and the number of binding sites was 35.5 fmol/mg protein. Since methyltrienolone also binds glucocorticoid receptor which exists in rat liver, the apparent binding of androgen receptor is faulty when measured in the presence of glucocorticoid receptor. The binding of methyltrienolone to glucocorticoid receptor can be blocked by the presence of a 100-fold molar excess of unlabeled synthetic glucocorticoid, triamcinolone acetonide, without interfering in its binding to androgen receptor, because triamcinolone does not bind to androgen receptor. Triamcinolone-blocked cytosol exhibited that the Kd value was 2.5 X 10(-8) M and the number of binding sites was 26.3 fmol/mg protein, indicating a reduction to 3/4 of that in the untreated cytosol. The profile of glycerol gradient centrifugation indicated that [3H]methyltrienolone-bound receptor migrated in the 8-9 S region in both untreated and triamcinolone-blocked cytosols, but the 8-9 S peak in triamcinolone-blocked cytosol was reduced to about 3/4 of that of untreated cytosol. SN - 0006-3002 UR - https://www.unboundmedicine.com/medline/citation/6331850/Binding_of_[3H]methyltrienolone_to_androgen_receptor_in_rat_liver_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0304-4165(84)90398-2 DB - PRIME DP - Unbound Medicine ER -