Manz B, Hoffmann G, Heubner A, Grill H J, Pollow K
J Steroid Biochem. 1984 Oct;21(4):427-32. doi: 10.1016/0022-4731(84)90306-6.
The present report describes an assay system allowing the quantification and characterization of [3H]cortisol binding to glucocorticoid receptors in bloodrich human tissue. The essence of this assay lies in the selective binding of 17 beta-carboxylic acids of natural corticoids to corticosteroid binding globulin (CBG). In the presence of 1240 nmol/l 11 beta-hydroxy-3-oxo-4-androstene-17 beta-carboxylic acid only glucocorticoid receptors were detectable with the expected properties: high affinity for synthetic and natural glucocorticoids, but failure to bind to the respective 17 beta-carboxylic acids, apparent Kd's at 0-4 degrees C for [3H]cortisol of approx 30 nmol/l, Nmax similar to those determined with [3H]dexamethasone and the typical sequence of relative binding affinities (dexamethasone greater than cortisol greater than progesterone greater than 17 beta-methyl-testosterone, estradiol).
本报告描述了一种检测系统，该系统可对富含血液的人体组织中[³H]皮质醇与糖皮质激素受体的结合进行定量和表征。该检测方法的核心在于天然皮质激素的17β - 羧酸与皮质类固醇结合球蛋白（CBG）的选择性结合。在1240 nmol/L的11β - 羟基 - 3 - 氧代 - 4 - 雄烯 - 17β - 羧酸存在的情况下，仅能检测到具有预期特性的糖皮质激素受体：对合成和天然糖皮质激素具有高亲和力，但不能与相应的17β - 羧酸结合，在0 - 4℃时[³H]皮质醇的表观解离常数（Kd）约为30 nmol/L，最大结合容量（Nmax）与用[³H]地塞米松测定的相似，且具有典型的相对结合亲和力顺序（地塞米松＞皮质醇＞孕酮＞17β - 甲基睾酮＞雌二醇）。
