Agarwal M K
Hormone Laboratory, Centre Universitaire des Cordeliers, Paris.
Naturwissenschaften. 1994 Mar;81(3):115-22. doi: 10.1007/BF01131766.
Receptor stabilization, activation, dimerization, and binding to cognate sequences on DNA are possible with antagonists. Tissue-, steroid-, and species-dependent differences in all these parameters, despite identical structure of the receptor from various sources for any one steroid hormone class, suggest posttranslational modifications of a primary gene product. Clinically, it is now possible to visualize receptor-specific antihormone therapy of various steroid-dependent maladies (cancer of the breast, uterus, or prostate, Cushing's disease, hypertensive disorders, etc.) where surgical resection has been hitherto most effective. Amelioration of adverse side effects, associated with currently available semispecific derivatives, should permit wider applications in a variety of other situations in the near future.
拮抗剂可实现受体的稳定、激活、二聚化以及与DNA上同源序列的结合。尽管对于任何一类甾体激素，来自不同来源的受体结构相同，但所有这些参数在组织、甾体和物种方面存在差异，这表明初级基因产物存在翻译后修饰。临床上，目前已能够可视化各种甾体依赖性疾病（乳腺癌、子宫癌或前列腺癌、库欣病、高血压疾病等）的受体特异性抗激素治疗，此前手术切除一直是最有效的治疗方法。与目前可用的半特异性衍生物相关的不良副作用的改善，应能在不久的将来在各种其他情况下得到更广泛的应用。
