Svec F, Teubner V, Tate D
Louisiana State University Medical Center, Department of Medicine, New Orleans 70112.
J Recept Res. 1989;9(4-5):405-14. doi: 10.3109/10799898909066066.
The physico-chemical properties of glucocorticoid receptors bound with tritiated corticosterone were compared to those of the triamcinolone acetonide glucocorticoid receptor complex. The goal was to determine whether the natural agonist forms complexes similar to those generated by the synthetic agonist. Structure was probed using three techniques; diethylaminoethyl-cellulose (DEAE) chromatography, vertical tube rotor sucrose gradient ultracentrifugation (SGU) and high performance liquid chromatography (HPLC). These techniques are all fast enough to allow analysis of the labile corticosterone receptor complexes. Results showed that complexes generated by both classes of ligands were similar. They eluted from DEAE cellulose and HPLC columns at similar positions and sedimented similarly in sucrose gradients. This was true for both the untransformed and transformed species. It is concluded that natural and synthetic glucocorticoid agonists interact with glucocorticoid receptors to form indistinguishable complexes. Thus synthetic agonists are appropriate probes of events which take place with natural glucocorticoids.
将与氚化皮质酮结合的糖皮质激素受体的物理化学性质与曲安奈德糖皮质激素受体复合物的性质进行了比较。目的是确定天然激动剂形成的复合物是否与合成激动剂产生的复合物相似。使用三种技术探测结构：二乙氨基乙基纤维素（DEAE）色谱、垂直管转子蔗糖梯度超速离心（SGU）和高效液相色谱（HPLC）。这些技术都足够快，能够分析不稳定的皮质酮受体复合物。结果表明，两类配体产生的复合物相似。它们从DEAE纤维素和HPLC柱上的洗脱位置相似，在蔗糖梯度中的沉降也相似。未转化和转化的物种都是如此。结论是天然和合成糖皮质激素激动剂与糖皮质激素受体相互作用形成难以区分的复合物。因此，合成激动剂是研究天然糖皮质激素发生事件的合适探针。
