Bhakoo H S, Milholland R J, Lopez R, Karakousis C, Rosen F
J Natl Cancer Inst. 1981 Jan;66(1):21-5.
The glucocorticoid receptor was characterized in biopsy samples from patients with recurrent malignant melanoma. Glucocorticoid receptors were measured by the charcoal-adsorption technique. Tumor cytosol from approximately 86% (25/29) of the patients contained large quantities of receptors (20-324 fmol/mg protein). The dissociation constant of this cytoplasmic receptor was determined to be 2-22 nM. This binding component sedimented at 7.1S on sucrose gradients of low ionic strength and dissociated into lower molecular weight components that sedimented at 4.4S on sucrose gradients of high ionic strength. Receptor binding was specific for glucocorticoids. Although progestins competed well for the binding that is typical for glycocorticoid receptor as reported in the literature, other steroids, e.g., 17 beta-estradiol and 5 alpha-dihydrotestosterone, were only weak competitors. These results demonstrated that this neoplasm contains large quantities of glucocorticoid receptors that are similar in their physicochemical characteristics to those found in normal tissues. This finding in human melanoma biopsy specimens may be of therapeutic value in the management of patients with malignant melanoma.
在复发性恶性黑色素瘤患者的活检样本中对糖皮质激素受体进行了表征。通过活性炭吸附技术测量糖皮质激素受体。约86%(25/29)患者的肿瘤胞质溶胶含有大量受体(20 - 324 fmol/mg蛋白质)。该细胞质受体的解离常数测定为2 - 22 nM。此结合成分在低离子强度的蔗糖梯度中沉降系数为7.1S,并在高离子强度的蔗糖梯度中解离成沉降系数为4.4S的较低分子量成分。受体结合对糖皮质激素具有特异性。尽管孕激素如文献报道的那样能很好地竞争糖皮质激素受体典型的结合,但其他类固醇,如17β - 雌二醇和5α - 双氢睾酮,只是弱竞争者。这些结果表明,这种肿瘤含有大量糖皮质激素受体,其物理化学特性与正常组织中的相似。在人类黑色素瘤活检标本中的这一发现可能对恶性黑色素瘤患者的治疗具有价值。