Kontula K, Paavonen T, Vuopio P, Andersson L C
Int J Cancer. 1982 Oct 15;30(4):423-6. doi: 10.1002/ijc.2910300407.
Glucocorticoid receptors were measured from leukemic cells of five patients with hairy-cell leukemia as well as a cell line (JOK-1) derived from one of the patients studied and grown in continuous culture in vitro. Receptor analyses were accomplished using a whole-cell binding assay with [3H]dexamethasone as the ligand. Glucocorticoid receptor sites in the leukemic hairy cells ranged from 5,710 to 11,400 sites/cell, and the mean dissociation constant (KD) between the receptor sites and [3H]dexamethasone was 0.67 +/- 0.03 X 10(-8) M. The glucocorticoid receptor nature of the binding activity was verified by demonstration of an appropriate order of competing ability for a selected group of ligands. The cell line JOK-1 contained 9830 receptor sites/cell with a KD of 0.78 X 10(-8) M. The in vitro growth pattern of this cell line was characterized by an almost complete insensitivity to glucocorticoids. We conclude that the postulated general presence of glucocorticoid receptors in various types of normal and malignant leukocytes extends to hairy-cell leukemia, a disease often characterized by resistance to antileukemic drugs, including corticosteroids. The sole presence of the glucocorticoid receptor thus does not seem to signify steroid responsiveness.
对5例毛细胞白血病患者的白血病细胞以及从其中1例患者分离并在体外连续培养的细胞系(JOK-1)进行了糖皮质激素受体检测。受体分析采用以[3H]地塞米松为配体的全细胞结合试验完成。白血病毛细胞中的糖皮质激素受体位点为5710至11400个/细胞,受体位点与[3H]地塞米松之间的平均解离常数(KD)为0.67±0.03×10(-8)M。通过对一组选定配体的竞争能力展示出适当顺序,证实了结合活性的糖皮质激素受体性质。细胞系JOK-1含有9830个受体位点/细胞,KD为0.78×10(-8)M。该细胞系的体外生长模式特点是对糖皮质激素几乎完全不敏感。我们得出结论,假定各种类型正常和恶性白细胞中普遍存在糖皮质激素受体这一情况也适用于毛细胞白血病,该病通常以对包括皮质类固醇在内的抗白血病药物耐药为特征。因此,仅存在糖皮质激素受体似乎并不意味着对类固醇有反应。