Kinase modulation of androgen receptor signaling: implications for prostate cancer.
Kinase modulation of androgen receptor signaling: implications for prostate cancer.
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DOI：
10.14800/ccm.1023
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发表时间：
2015-01-01
期刊：
影响因子：
--
通讯作者：
Bradbury, Neil A
中科院分区：
文献类型：
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作者：
Shah, Kalpit;Bradbury, Neil A
雄激素和雄激素受体在前列腺癌的发展和进展中起着至关重要的作用，前列腺癌是一种每年夺去大约28，000人生命的疾病。除了雄激素结合外，雄激素受体活性还可以通过几种翻译后修饰来调节，如泛素化、乙酰化、磷酸化、甲基化和SUMO-化。在这些修饰中，磷酸化被最广泛地研究。通过磷酸化修饰可以改变雄激素受体定位、蛋白质稳定性和转录活性，最终导致癌细胞生物学的变化和癌症进展。了解磷酸化雄激素受体种类的作用是确定前列腺癌和去势抵抗性前列腺癌患者的潜在治疗药物靶点的关键。在这里，我们提出了一个简短的审查，最近发现的蛋白激酶磷酸化AR，集中在前列腺癌和去势抵抗性前列腺癌的功能作用的磷酸化雄激素受体物种。
Androgens and androgen receptors play essential roles in the development and progression of prostate cancer, a disease that claims roughly 28,000 lives annually. In addition to androgen biding, androgen receptor activity can be regulated via several post-translational modifications such as ubiquitination, acetylation, phosphorylation, methylation & SUMO-ylation. Off these modifications, phosphorylation has been the most extensively studied. Modification by phosphorylation can alter androgen receptor localization, protein stability and transcriptional activity, ultimately leading to changes in the biology of cancer cells and cancer progression. Understanding, role of phosphorylated androgen receptor species holds the key to identifying a potential therapeutic drug target for patients with prostate cancer and castrate resistant prostate cancer. Here, we present a brief review of recently discovered protein kinases phosphorylating AR, focusing on the functional role of phosphorylated androgen receptor species in prostate cancer and castrate resistant prostate cancer.