Geier A, Ginzburg R, Stauber M, Lunenfeld B
J Endocrinol. 1979 Mar;80(3):281-8. doi: 10.1677/joe.0.0800281.
The binding of oestradiol to a nuclear fraction extracted from human breast carcinomatous tissue was demonstrated. The material, which was extracted with KCl, sedimented at 3--4S and bound oestradiol with high affinity (dissociation constant approximately 2 X 10(-10) mol/l). Oestriol, diethylstilboestrol and 5 alpha-dihydrotestosterone (100-fold excesses) competed with [3H]oestradiol for the binding sites (binding inhibited by 89 +/- 8 (S.D.), 92 +/- 6 and 57 +/- 8% respectively), whereas progesterone and cortisol (100-fold excesses) did not (binding suppressed by 5 +/- 5 and 2 +/- 3% respectively). Similar competition patterns were found for cytoplasmic material which bound oestradiol. The binding occurred at 4 degrees C and was therefore considered to be a measure of the amount of binding material unoccupied by endogenous oestrogen, Unoccupied binding sites for oestradiol in the nucleus and cytoplasm were measured in 35 samples of breast carcinomatous tissue using sucrose gradient centrifugation. In 17 out of 35 tumorus, unoccupied nuclear and cytoplasmic 8S and 4S binding sites could be detected. Three out of 35 tumours contained unoccupied nuclear binding sites and 4S cytoplasmic binding sites. Nuclear binding sites only were found in two out of 35 tumours. Unoccupied nuclear binding sites were not detected in 13 out of 35 tumours and ten of these tumours also did not contain unoccupied cytoplasmic binding sites.
已证实雌二醇与人乳腺癌组织提取的核部分具有结合能力。该物质用氯化钾提取，在3 - 4S处沉降，并以高亲和力结合雌二醇（解离常数约为2×10⁻¹⁰mol/L）。雌三醇、己烯雌酚和5α - 双氢睾酮（过量100倍）与[³H]雌二醇竞争结合位点（结合分别被抑制89±8（标准差）、92±6和57±8%），而孕酮和皮质醇（过量100倍）则无此作用（结合分别被抑制5±5和2±3%）。对于结合雌二醇的细胞质物质也发现了类似的竞争模式。结合在4℃时发生，因此被认为是内源性雌激素未占据的结合物质数量的一种度量。使用蔗糖梯度离心法在35份乳腺癌组织样本中测量了细胞核和细胞质中未占据的雌二醇结合位点。在35个肿瘤样本中，有17个可检测到未占据的细胞核和细胞质8S及4S结合位点。35个肿瘤中有3个含有未占据的细胞核结合位点和4S细胞质结合位点。35个肿瘤中仅有2个发现了细胞核结合位点。35个肿瘤中有13个未检测到未占据的细胞核结合位点，其中10个肿瘤也不含有未占据的细胞质结合位点。
