Resistance emerges to second-generation antiandrogens in prostate cancer.

Resistance emerges to second-generation antiandrogens in prostate cancer.
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DOI:
10.1158/2159-8290.cd-13-0405
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发表时间:
2013-09
期刊:
影响因子:
28.2
通讯作者:
Yegnasubramanian S
Yegnasubramanian S
中科院分区:
医学1区
文献类型:
--
作者:
Nelson WG;Yegnasubramanian S

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在长期暴露于苯扎鲁胺或ARN-509的前列腺癌细胞中,突变的雄激素受体F876L-AR的出现促进了从拮抗剂到激动剂受体功能的转换,破坏了这些第二代抗雄激素药物的潜在长期有效性。
The appearance of a mutant androgen receptor, F876L-AR, in prostate cancer cells chronically exposed to enzalutamide or ARN-509 promotes a switch from antagonist to agonist receptor function, undermining the potential long term effectiveness of these second generation anti-androgen drugs.