The fluorescent two-hybrid assay for live-cell profiling of androgen receptor modulators

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• 作者：Jacqueline Bogner^a ; Kourosh Zolghadr^a ; Ian Hickson^b ; Tina Romer^a ; ^{t.romer@chromotek.com} ; Larisa Yurlova^a
• 关键词：AR ; androgen receptor protein ; BHK ; baby hamster kidney ; CMV IE ; immediate early promoter of cytomegalovirus ; CRPC ; castration resistant prostate cancer ; CYP17 ; 17α-hydroxy/17 ; 20-lyase ; DAPI ; 4&prime ; 6-diamidino-2-phenylindole ; DBD ; DNA-binding domain ; DHT ; 5α-dihydrotestosterone ; DMEM ; Dulbecco&rsquo ; s Modified Eagle Medium ; DNA ; deoxyribonucleic acid ; F2H ; fluorescent two-hybrid ; FDA ; Food and Drug Administration ; GFP ; green fluorescent protein ; HCA ; high-content analysis ; HEK ; human embryoni
• 刊名：The Journal of Steroid Biochemistry and Molecular Biology
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：166
• 期：Complete
• 页码：45-53
• 全文大小：1332 K
• 卷排序：166

文摘

F2H AR is a novel live-cell assay for evaluation of androgens and antiandrogens. DHT, abiraterone, bicalutamide, enzalutamide, flutamide, galeterone were tested. W741L, F876L, T877A and F876L/T877A AR mutations were evaluated with F2H AR. The assay enables real-time visualization and monitoring of compounds’ activity. The assay facilitates comparative analysis of mutant AR activation upon treatments.