Ojasoo T, Doré J C, Gilbert J, Raynaud J P
Roussel-Uclaf, Paris, France.
J Med Chem. 1988 Jun;31(6):1160-9. doi: 10.1021/jm00401a015.
The relative binding affinities of over 30 steroids have been measured for the cytosol glucocorticoid receptor (GR) of thymus, liver, and hepatoma tissue culture cells and for progestin, androgen, and mineralocorticoid receptors. The data have been analyzed by correspondence analysis to reveal the singularities among the receptors of different hormonal classes, the similarities in GR of different origins, and the different specificities of the ligands. Additional data on new steroids have been injected into the system as well as results on a further parameter, namely the induction of tyrosine aminotransferase (TAT) activity, to illustrate the power and flexibility of the methodology. The analysis has confirmed previous correlations between GR binding and TAT response but also highlighted the antiglucocorticoid activity of progestins. This method should prove to be a substantial aid to the interpretation of increasingly complex data, in particular with regard to the action of existing and newly synthesized steroids on glucocorticoid systems of differential sensitivity.
已测定了30多种甾体激素对胸腺、肝脏和肝癌组织培养细胞的胞质溶胶糖皮质激素受体(GR)以及孕激素、雄激素和盐皮质激素受体的相对结合亲和力。通过对应分析对数据进行了分析,以揭示不同激素类别受体之间的独特性、不同来源GR的相似性以及配体的不同特异性。新甾体激素的其他数据以及另一个参数(即酪氨酸转氨酶(TAT)活性的诱导)的结果也已输入该系统,以说明该方法的强大功能和灵活性。该分析证实了先前GR结合与TAT反应之间的相关性,但也突出了孕激素的抗糖皮质激素活性。该方法应被证明对解释日益复杂的数据有很大帮助,特别是在现有和新合成的甾体激素对不同敏感性的糖皮质激素系统的作用方面。