Jordan V C, Prestwich G
Mol Cell Endocrinol. 1977 Sep;8(3):179-88. doi: 10.1016/0303-7207(77)90090-9.
The interaction of the antioestrogen tamoxifen with rat uterine oestrogen receptor has been studied using swinging bucket and vertical tube rotor techniques of sucrose density gradient analysis. Tamoxifen inhibits the binding of [3H]oestradiol to the 8S oestrogen receptor protein whereas using the swinging bucket rotor technique of sucrose density gradient analysis [3H]-tamoxifen appears to bind to an oestradiol specific protein which sediments at 4-5S. In contrast, using rapid sucrose density gradient analysis with a vertical tube rotor [3H]tamoxifen shows oestrogen specific binding in the 8S region. It is suggested that conventional techniques of sucrose density gradient analysis are unsuited for the investigation of the low affinity ligand interactions with oestrogen receptor proteins since rapid dissociation of complexes can result in ligand binding to nonreceptor proteins.
已使用蔗糖密度梯度分析的摆动桶和垂直管转子技术研究了抗雌激素他莫昔芬与大鼠子宫雌激素受体的相互作用。他莫昔芬抑制[3H]雌二醇与8S雌激素受体蛋白的结合，而使用蔗糖密度梯度分析的摆动桶转子技术时，[3H]他莫昔芬似乎与一种沉降系数为4 - 5S的雌二醇特异性蛋白结合。相比之下，使用垂直管转子进行快速蔗糖密度梯度分析时，[3H]他莫昔芬在8S区域显示出雌激素特异性结合。有人提出，传统的蔗糖密度梯度分析技术不适用于研究低亲和力配体与雌激素受体蛋白的相互作用，因为复合物的快速解离会导致配体与非受体蛋白结合。
