TY - JOUR
T1 - Hormone receptors of the baboon cardiovascular system. Biochemical characterization of myocardial cytoplasmic androgen receptors
AU - Lin, A. L.
AU - McGill, H. C.
AU - Shain, S. A.
PY - 1981
Y1 - 1981
N2 - Using the synthetic androgen R1881 (17β-hydroxy-17α-methyl-estra-4,9,11-trien-3-one) as probe, we identified cytoplasmic androgen receptors in baboon myocardium. The relative binding affinity of selected steroids for the androgen receptor was R1881, 100%; 5α-dihydrotestosterone, 32.6%; testosterone, 29.6%, progesterone, 7.2%; R5020, 1.0%; and estradiol-17β, 5.8%. The androgen receptor migrated on low ionic strength linear sucrose density gradients as a macromolecule with a sedimentation coefficent of 8.5S. Saturation analysis performed at 2°C (available sites) showed that the androgen receptor content of baboon myocardial cytoplasmic extracts were 5.9 ± 1.4 fmol/mg protein and that the dissociation constant for R1881 was 1.16 ± 0.30 nM. These cytoplasmic androgen receptors are indicated to be physiologically functional by previous autoradiographic studies (McGill et al., 1980; McGill and Sheridan, 1981) that showed localization of radioisotope in nuclei of myocardial fibers following injection of baboons with 5α-dihydrotestosterone.
AB - Using the synthetic androgen R1881 (17β-hydroxy-17α-methyl-estra-4,9,11-trien-3-one) as probe, we identified cytoplasmic androgen receptors in baboon myocardium. The relative binding affinity of selected steroids for the androgen receptor was R1881, 100%; 5α-dihydrotestosterone, 32.6%; testosterone, 29.6%, progesterone, 7.2%; R5020, 1.0%; and estradiol-17β, 5.8%. The androgen receptor migrated on low ionic strength linear sucrose density gradients as a macromolecule with a sedimentation coefficent of 8.5S. Saturation analysis performed at 2°C (available sites) showed that the androgen receptor content of baboon myocardial cytoplasmic extracts were 5.9 ± 1.4 fmol/mg protein and that the dissociation constant for R1881 was 1.16 ± 0.30 nM. These cytoplasmic androgen receptors are indicated to be physiologically functional by previous autoradiographic studies (McGill et al., 1980; McGill and Sheridan, 1981) that showed localization of radioisotope in nuclei of myocardial fibers following injection of baboons with 5α-dihydrotestosterone.
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U2 - 10.1161/01.RES.49.4.1010
DO - 10.1161/01.RES.49.4.1010
M3 - Article
C2 - 6268332
AN - SCOPUS:0019520722
VL - 49
SP - 1010
EP - 1016
JO - Circulation Research
JF - Circulation Research
SN - 0009-7330
IS - 4
ER -