McPartland R P, Milholland R J, Morris H P, Rosen F
Cancer Res. 1977 Nov;37(11):4160-5.
Glucocorticoid-binding macromolecules were examined in Morris hepatomas 7787, 5123tc, 3683F, 7800, and 3683 and the Reuber hepatoma H-35 with the use of the synthetic glucocorticoid, triamcinolone acetonide. The physical properties of the triamcinolone acetonide-binding macromolecules of the hepatomas indicate that they are specific glucocorticoid receptors. The equilibrium association constants (Ka), sedimentation coefficients, and sensitivity to sulfhydryl-blocking reagents were found to be similar when hepatoma receptors were compared with the known properties of the liver receptor. Probably the most convincing criterion that the triamcinolone acetonide-binding macromolecules from the hepatomas are specific receptors is that 50 to 90% of the receptor can be depleted from hepatoma cytosol by treating rats with cortisol. In adrenalectomized tumor-bearing rats, the receptor levels in hepatomas 7787, 7800, 5123tc, and H-35 are comparable to or greater than receptor levels of host liver. However, tryptophan oxygenase was not responsive to glucocorticoids in hepatoma 7800 although receptor levels were quite high, and there were no indications that the receptor molecules were altered. Hepatomas 3683 and 3686F have low levels of receptor which may be related to resistance of these tumors to glucocorticoid treatment.
利用合成糖皮质激素曲安奈德，对莫里斯肝癌7787、5123tc、3683F、7800、3683以及鲁伯肝癌H - 35中的糖皮质激素结合大分子进行了检测。肝癌中曲安奈德结合大分子的物理性质表明它们是特异性糖皮质激素受体。将肝癌受体与肝脏受体的已知特性进行比较时，发现平衡缔合常数（Ka）、沉降系数以及对巯基阻断试剂的敏感性相似。肝癌中曲安奈德结合大分子是特异性受体这一点，可能最最有说服力的标准可能是，通过用皮质醇处理大鼠，肝癌细胞溶质中50%至90%的受体可被耗尽。在肾上腺切除的荷瘤大鼠中，肝癌7787、7800、5123tc和H - 35中的受体水平与宿主肝脏的受体水平相当或更高。然而，尽管肝癌7800中的受体水平相当高，但其色氨酸加氧酶对糖皮质激素无反应，且没有迹象表明受体分子发生了改变。肝癌3683和3686F的受体水平较低，这可能与这些肿瘤对糖皮质激素治疗的抗性有关。
