Dmitrieva L V, Volchek A G, Rozen V B, Adler V V, Shapot V S
Biokhimiia. 1976 Oct;41(10):1850-8.
Specific dexametasone (D) and cortisol (F) receptors have been found both in liver and Zajdela hepatoma. Rat liver cytosol receptors are characterized by the association constant (Kas) = 3,8 X 10(8) M-1 for D and 0,57 X 10(8) M-1 for F as well as by a number of binding sites (NBS)=4,9 X 10(-13) moles/mg protein and 4,06 X 10(-13) moles/mg protein, respectively. The receptors show stric specificity to glucocorticoids. Cytosol glucocorticoid-receptor complexes from liver and hepatoma sediment at 6-7S, when centrifuged in the buffer of a low ionic strength, and at 3-4S in the buffer of a high ionic strength (0,4 M KCl). The properties of cytosol receptors in the course of in vivo hepatoma growth were found to be gradually altering: Kas for D dropped whereas that for F increased; the NBS is decreased 3-4 fold as compared to normal liver cytosol--which may partially be accounted for by the unresponsiveness of the tumour to the hormones.
在肝脏和Zajdela肝癌中均已发现特异性地塞米松（D）受体和皮质醇（F）受体。大鼠肝脏胞质溶胶受体的特征在于，地塞米松的缔合常数（Kas）= 3.8×10⁸ M⁻¹，皮质醇的缔合常数为0.57×10⁸ M⁻¹，以及结合位点数（NBS）分别为4.9×10⁻¹³摩尔/毫克蛋白质和4.06×10⁻¹³摩尔/毫克蛋白质。这些受体对糖皮质激素表现出严格的特异性。当在低离子强度缓冲液中离心时，来自肝脏和肝癌的胞质溶胶糖皮质激素 - 受体复合物在6 - 7S沉降，而在高离子强度（0.4 M KCl）缓冲液中在3 - 4S沉降。发现在体内肝癌生长过程中胞质溶胶受体的性质逐渐改变：地塞米松的Kas下降而皮质醇的Kas增加；与正常肝脏胞质溶胶相比，NBS减少3 - 4倍，这可能部分是由于肿瘤对激素无反应所致。
