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Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer 期刊论文

编号：

41d6c7d7-9efd-41d6-8ecd-07fac54fa4c8
作者：

He, Yundong#^[1,2,3]Peng, Shihong#^[1,2,3]Wang, Jinhua#^[1,2,3]Chen, Huang^[1,2,3];Cong, Xiaonan^[1,2,3];Chen, Ang^[1,2,3];Hu, Meichun^[1,2,3];Qin, Min^[1,2,3];Wu, Haigang^[1,2,3];Gao, Shuman^[1,2,3];Wang, Liguo^[4];Wang, Xin*^[1,2,3]Yi, Zhengfang*^[1,2,3]Liu, Mingyao*^[1,2,3,5]
语种：

英文
期刊：

NATURE COMMUNICATIONS ISSN：2041-1723 2016 年 7 卷 ; DEC 13
收录：
摘要：

Androgen receptor (AR) antagonist MDV3100 is the first therapeutic approach in treating castration-resistant prostate cancer (CRPC), but tumours frequently become drug resistant via multiple mechanisms including AR amplification and mutation. Here we identify the small molecule Ailanthone (AIL) as a potent inhibitor of both full-length AR (AR-FL) and constitutively active truncated AR splice variants (AR-Vs). AIL binds to the co-chaperone protein p23 and prevents AR"s interaction with HSP90, thus resulting in the disruption of the AR-chaperone complex followed by ubiquitin/proteasome-mediated degradation of AR as well as other p23 clients including AKT and Cdk4, and downregulates AR and its target genes in PCa cell lines and orthotopic animal tumours. In addition, AIL blocks tumour growth and metastasis of CRPC. Finally, AIL possesses favourable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition and low hepatotoxicity. In general, AIL is a potential candidate for the treatment of CRPC.
推荐引用方式
GB/T 7714：

He Yundong,Peng Shihong,Wang Jinhua, et al. Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer [J].NATURE COMMUNICATIONS,2016,7.
APA：

He Yundong,Peng Shihong,Wang Jinhua,Chen Huang,&Liu Mingyao.(2016).Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer .NATURE COMMUNICATIONS,7.
MLA：

He Yundong, et al. "Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer" .NATURE COMMUNICATIONS 7(2016).
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