Discovery of nonsteroidal androgens
Discovery of nonsteroidal androgens
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DOI：
10.1006/bbrc.1998.8209
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发表时间：
1998-03-06
影响因子：
3.1
通讯作者：
Miller, DD
中科院分区：
文献类型：
--
作者：
Dalton, JT;Mukherjee, A;Miller, DD
非甾体雄激素尚未报道。在我们实验室的雄激素受体的亲和配体的研究，以确定，我们合成了几个亲电子的雄激素受体的非甾体配体，并检查其受体结合亲和力和能力，刺激受体介导的转录激活。我们发现这些配体中的三种（1）以与二氢睾酮（内源性配体）相似的亲和力结合雄激素受体，（2）模拟二氢睾酮对受体介导的转录激活的作用（即，它们是受体激动剂）。这些研究表明，非甾体配体可以进行结构修饰，产生激动剂活性。因此，这些配体代表了一类新型雄激素的第一个成员，在男性生育和激素替代疗法中具有潜在的治疗应用。(C)北京：科学出版社.
Nonsteroidal androgens have not been reported. During studies to identify affinity ligands for the androgen receptor in our laboratory, we synthesized several electrophilic nonsteroidal ligands for the androgen receptor and examined their receptor binding affinity and ability to stimulate receptor-mediated transcriptional activation. We found that three of these ligands (1) bound the androgen receptor with affinity similar to that of dihydrotestosterone (the endogenous ligand) and (2) mimicked the effects of dihydrotestosterone on receptor-mediated transcriptional activation (i.e., they were receptor agonists). These studies demonstrate that nonsteroidal ligands can be structurally modified to produce agonist activity. These ligands thus represent the first members of a novel class of androgens with potential therapeutic applications in male fertility and hormone replacement therapy. (C) 1998 Academic Press.