Emerging data on androgen receptor splice variants in prostate cancer.
Emerging data on androgen receptor splice variants in prostate cancer.
复制标题
前列腺癌中雄激素受体剪接变异的新兴数据。
DOI：
10.1530/erc-16-0298
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发表时间：
2016-12
影响因子：
3.9
通讯作者：
Dong Y
中科院分区：
文献类型：
--
作者：
Cao S;Zhan Y;Dong Y
雄激素受体剪接变体是雄激素受体的选择性剪接变体，其C末端截短并且缺乏典型配体结合结构域。越来越多的证据表明，雄激素受体剪接变异体在介导去势抵抗性前列腺癌对当前治疗的耐药性和预测治疗反应方面发挥着重要作用。因此，迫切需要靶向雄激素受体剪接变体以更有效地治疗去势抵抗性前列腺癌。确定精确和关键的靶点，以灭活雄激素受体剪接变体依赖于对它们如何产生及其作用机制的深入理解。在这篇综述中，我们将重点关注其产生，临床意义和作用机制以及这些发现的治疗影响的新数据。
Androgen receptor splice variants are alternatively spliced variants of androgen receptor that are C-terminally truncated and lack the canonical ligand-binding domain. Accumulating evidence has indicated a significant role of androgen receptor splice variants in mediating resistance of castration-resistant prostate cancer to current therapies and in predicting therapeutic responses. As such, there is an urgent need to target androgen receptor splicing variants for more effective treatment of castration-resistant prostate cancer. Identification of precise and critical targeting points to deactivate androgen receptor splicing variants relies on a deep understanding of how they are generated and the mechanisms of their action. In this review, we will focus on the emerging data on their generation, clinical significance, and mechanisms of action as well as the therapeutic impact of these findings.