The binding of a potent synthetic androgen--methyltrienolone (R 1881)--to cytosol preparations of human prostatic cancer.

P C Walsh, J M Greco, C E Tananis, L L Hicks, M G McLoughlin, M Menon
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Abstract

The binding of 3H-R 1881 to cytosol prepared from benign and malignant prostatic neoplasms has been investigated. We have demonstrated that high affinity binding of 3H-R 1881 is present in cytosol preparations of benign prostatic hyperplasia, in specimens of prostatic cancer obtained from patients prior to hormonal therapy and in carcinoma of the prostate metastatic to lymph nodes. In addition, high affinity binding was present in all specimens of prostatic cancer from patients who had objective evidence of progressive metastatic disease after an initial response to hormonal therapy. Until greater numbers of patients have been studied the significance of these findings can only be speculative. Because the binding of 3H-R 1881 may measure androgen and progesterone receptors future investigations must include careful steroid specificity studies. Finally, because steroidal hormones exert their major influence within the nucleus of target tissues the measurement of nuclear receptor content may provide a more accurate means to predict the hormonal responsiveness of prostatic cancer.

一种强效合成雄激素甲基三烯诺酮(r1881)与人类前列腺癌细胞质制剂的结合。
研究了3h - r1881与良恶性前列腺肿瘤细胞质的结合。我们已经证明3H-R 1881的高亲和力结合存在于良性前列腺增生的细胞质制剂中,在激素治疗前获得的前列腺癌标本中,以及转移到淋巴结的前列腺癌中。此外,高亲和力结合存在于所有前列腺癌标本中,这些患者在激素治疗的初始反应后有进展性转移性疾病的客观证据。在对更多的患者进行研究之前,这些发现的意义只能是推测性的。因为3H-R 1881的结合可以测量雄激素和孕激素受体,未来的研究必须包括仔细的类固醇特异性研究。最后,由于类固醇激素在靶组织的细胞核内发挥其主要影响,核受体含量的测量可能为预测前列腺癌的激素反应提供更准确的手段。
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