Recent Androgen Receptor Antagonists in Prostate Cancer

被引：3
作者：
Lu, Xufang [1 ]
Dun, Kang [1 ]
Wang, Yang [1 ]
Yang, Yong [2 ]
You, Qidong [1 ]
Li, Zhiyu [1 ]
机构：
[1] China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, Acad Inst Pharmaceut Sci, State Key Lab Nat Med, Nanjing 210009, Peoples R China
来源：
MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2014年 / 14卷 / 08期
基金：
中国国家自然科学基金;
关键词：
Androgen receptor; castration-resistant prostate cancer; prostate cancer; BIOLOGICAL EVALUATION; 17-BETA-HYDROXYSTEROID-DEHYDROGENASE AKR1C3; DESIGN; DERIVATIVES; INHIBITORS; DOMAIN; ACID;
D O I：
10.2174/1389557514666140622203207
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Androgen receptor has been shown to promote prostate cell growth and carcinogenesis of prostate cancer by up-regulating its target genes. Testosterone and dihydrotestosterone are two major hormones which bind to and activate androgen receptor. Targeting both the androgen receptor and the enzymes catalyzing the biosynthesis of testosterone and dihydrotestosterone has been shown to be clinically beneficial in the treatment of prostate cancer. Prostate cancer can become castration-resistant after long term treatment with chemo drugs, so efforts in finding compounds with improved efficiency to castration-resistant prostate cancer are urgently needed. In this review we summarized the studies on recent progress in the development of small molecular AR antagonists for the treatment of prostate cancer.
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页码：655 / 663
页数：9
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