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Review Article

非甾体雄激素受体拮抗剂和前列腺癌：结合该快速突变目标的化学结构的调查。

卷 26, 期 33, 2019

页: [6053 - 6073] 页: 21

弟呕挨: 10.2174/0929867325666180913095239

价格: $65

摘要

雄激素受体（AR）途径在前列腺癌的发病机理和进展中均起着重要作用。 特别是，AR主要参与去势抵抗性前列腺癌（CRPC）的开发，以及对第二代AR拮抗剂enzalutamide和细胞色素P450 17A1（CYP17A1）阿比特龙的选择性抑制剂的耐药性。 到目前为止，由于表达该分子靶标的细胞具有迅速发展抗性并将纯受体拮抗剂转变为无效或事件有害分子的能力，因此已经设计并开发了几种用作AR拮抗剂的小分子。 这篇综述涵盖了对最有前景的非甾体雄激素受体拮抗剂类别的调查，还提供了其对前列腺癌的作用机理和功效的见解。

关键词: 雄激素受体，去势抵抗性前列腺癌，抗雄激素，点突变，PROTAC，AR蛋白降解剂，靶向AR的结合物。

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