Bojar H, Maar K, Staib W
Urol Int. 1980;35(2):154-60. doi: 10.1159/000280315.
The binding of methyltrienolone (R 1881, 17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-trien-3-one), a highly active synthetic androgen, by cytosol preparations from human renal cell carcinoma was investigated. High-affinity, low-capacity binding components for R 1881 were detected in 3 out of 8 tumours analysed. The apparent dissociation constant of the R 1881-binder complexes was found to be in the range of 1.1-2.3 x 10(-9) mol/l. The number of binding sites in the positive tumours varied from 2.1 to 9.7 fmol/mg cytosol protein. Studies of binding specificity indicated a requirement for androgens. It is concluded that these binding components may be hormone receptors. If in consecutive studies this hypothesis holds true, progestins, most widely used in hormonal therapy of metastatic renal cancer, may possibly act on the tumour tissue by inhibiting the secretion of gonadotropins, thus lowering the blood levels of eventually growth-promoting.
研究了高活性合成雄激素甲基三烯醇酮（R1881，17β-羟基-17α-甲基-雌甾-4,9,11-三烯-3-酮）与人肾细胞癌胞浆制剂的结合情况。在分析的8个肿瘤中有3个检测到了R1881的高亲和力、低容量结合成分。R1881-结合物复合物的表观解离常数在1.1 - 2.3×10⁻⁹mol/L范围内。阳性肿瘤中结合位点的数量在2.1至9.7fmol/mg胞浆蛋白之间。结合特异性研究表明需要雄激素。结论是这些结合成分可能是激素受体。如果在后续研究中该假设成立，在转移性肾癌激素治疗中最广泛使用的孕激素可能通过抑制促性腺激素的分泌作用于肿瘤组织，从而降低最终可能促进生长的血液水平。
