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EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor

机译:EPI-001是一种对去势抵抗性前列腺癌有活性的化合物,它靶向雄激素受体的反式激活单元5

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摘要

Castration-resistant prostate cancer is the lethal condition suffered by prostate cancer patients that become refractory to androgen deprivation therapy. EPI-001 is a recently identified compound active against this condition that modulates the activity of the androgen receptor, a nuclear receptor that is essential for disease progression. The mechanism by which this compound exerts its inhibitory activity is however not yet fully understood. Here we show, by using high resolution solution nuclear magnetic resonance spectroscopy, that EPI-001 selectively interacts with a partially folded region of the transactivation domain of the androgen receptor, known as transactivation unit 5, that is key for the ability of prostate cells to proliferate in the absence of androgens, a distinctive feature of castration-resistant prostate cancer. Our results can contribute to the development of more potent and less toxic novel androgen receptor antagonists for treating this disease.
机译:抗去势抵抗性前列腺癌是对雄激素剥夺疗法难以治疗的前列腺癌患者所遭受的致死性疾病。 EPI-001是最近鉴定出的对这种病情具有活性的化合物,可调节雄激素受体(一种对疾病进展至关重要的核受体)的活性。然而,该化合物发挥其抑制活性的机理尚不完全清楚。在这里,我们显示通过使用高分辨率溶液核磁共振波谱,EPI-001与雄激素受体反式激活域的部分折叠区域(称为反式激活单元5)选择性相互作用,这对于前列腺细胞的功能至关重要。在没有雄激素的情况下增殖,这是去势抵抗性前列腺癌的显着特征。我们的结果可有助于开发更有效和毒性更低的新型雄激素受体拮抗剂来治疗该疾病。

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