A new dawn for androgens: Novel lessons from 11-oxygenated C19 steroids
A new dawn for androgens: Novel lessons from 11-oxygenated C19 steroids
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DOI：
10.1016/j.mce.2016.08.014
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发表时间：
2017-02-05
影响因子：
4.1
通讯作者：
Storbeck, Karl-Heinz
中科院分区：
文献类型：
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作者：
Pretorius, Elzette;Ark, Wiebke;Storbeck, Karl-Heinz
丰富的肾上腺 C19 类固醇 11β-羟基雄烯二酮 (11OA4) 已被视为肾上腺类固醇生成的最终产物。然而，最近的证据表明，11OHA4 是强效雄激素 11-氧化类固醇、11-酮睾酮和 11-酮二氢睾酮的前体，它们与睾酮和 DHT 类似，结合并激活人类雄激素受体。当考虑雄激素依赖性疾病（例如去势抵抗性前列腺癌）和与雄激素过多相关的疾病（例如前列腺癌）时，这一发现的重要性就变得显而易见。先天性肾上腺皮质增生症和多囊卵巢综合症。在这篇综述中，我们描述了 11-含氧类固醇的产生和代谢。我们随后讨论它们的雄激素活性，并强调这些雄激素在疾病状态中的假定作用。 (C) 2016 Elsevier Ireland Ltd. 保留所有权利。
The abundant adrenal C19 steroid 11 beta-hydroxyandrostenedione (11OA4) has been written off as a dead-end product of adrenal steroidogenesis. However, recent evidence has demonstrated that 11OHA4 is the precursor to the potent androgenic 11-oxygenated steroids, 11-ketotestosterone and 11-ketodihydrotestosterone, that bind and activate the human androgen receptor similarly to testosterone and DHT. The significance of this discovery becomes apparent when considering androgen dependent diseases such as castration resistant prostate cancer and diseases associated with androgen excess, e.g. congenital adrenal hyperplasia and polycystic ovary syndrome. In this review we describe the production and metabolism of 11-oxygenated steroids. We subsequently discuss their androgenic activity and highlight the putative role of these androgens in disease states. (C) 2016 Elsevier Ireland Ltd. All rights reserved.