TY - JOUR
T1 - Partial characterization of [3H]methyltrienolone binding in rat prostate cytosol
AU - Pousette, Åke
AU - Snochowski, Marek
AU - Bression, Dominique
AU - Högberg, Bertil
AU - Gustafsson, Jan Åke
N1 - Funding Information:
This work was supported by grants from LEO Research Foundation, from RiksfSreningen mot Cancer and from Svenska L~ikarestillskapet.
Copyright:
Copyright 2018 Elsevier B.V., All rights reserved.
PY - 1979/1/18
Y1 - 1979/1/18
N2 -
3H-labelled R 1881 (methyltrienolone) was bound with high affinity (Kd, 2 · 10-9 M) and low capacity (11-15 fmol/mg protein) in prostate cytosol from rats castrated 18 h earlier. The binding was inhibited by 5α-dihydrotosterone, testosterone, cyproterone acetate and LEO 1727, but not by estradiol-17β, R 5020 or corticosterone. The 3H-labelled R 1881-receptor complex was excluded from a Sephadex G-200 column, had a sedimentation coefficient of 3.5 S, was eluted from a DEAE-cellulose column at 0.2 M KCl concentration and precipitated between 20-40% of saturation of ammonium sulfate. 20% of specifically bound 3H-labelled R 1881 was retained by DNA-cellulose at low ionic strength. The fraction which was not bound to DNA-cellulose did not bind either, after rechromatography, not even following heating at 20°C for 20 min or following fractionation with ammonium sulphate. In summary, the results indicate that the 3H-labelled R 1881-receptor complex in rat prostate cytosol has characteristics similar to those of the 5μ-[3H]-dihydrotestosterone-receptor complex.
AB -
3H-labelled R 1881 (methyltrienolone) was bound with high affinity (Kd, 2 · 10-9 M) and low capacity (11-15 fmol/mg protein) in prostate cytosol from rats castrated 18 h earlier. The binding was inhibited by 5α-dihydrotosterone, testosterone, cyproterone acetate and LEO 1727, but not by estradiol-17β, R 5020 or corticosterone. The 3H-labelled R 1881-receptor complex was excluded from a Sephadex G-200 column, had a sedimentation coefficient of 3.5 S, was eluted from a DEAE-cellulose column at 0.2 M KCl concentration and precipitated between 20-40% of saturation of ammonium sulfate. 20% of specifically bound 3H-labelled R 1881 was retained by DNA-cellulose at low ionic strength. The fraction which was not bound to DNA-cellulose did not bind either, after rechromatography, not even following heating at 20°C for 20 min or following fractionation with ammonium sulphate. In summary, the results indicate that the 3H-labelled R 1881-receptor complex in rat prostate cytosol has characteristics similar to those of the 5μ-[3H]-dihydrotestosterone-receptor complex.
KW - (Rat prostate)
KW - Androgen receptor
KW - Methyltrienolone
UR - http://www.scopus.com/inward/record.url?scp=0018794808&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0018794808&partnerID=8YFLogxK
U2 - 10.1016/0304-4165(79)90397-0
DO - 10.1016/0304-4165(79)90397-0
M3 - Article
C2 - 760830
AN - SCOPUS:0018794808
VL - 582
SP - 358
EP - 367
JO - Biochimica et Biophysica Acta - General Subjects
JF - Biochimica et Biophysica Acta - General Subjects
SN - 0304-4165
IS - 2
ER -