Literature DB >> 17219378

Rapid, non-destructive, cell-based screening assays for agents that modulate growth, death, and androgen receptor activation in prostate cancer cells.

Peyman Tavassoli1, Rob Snoek, Mira Ray, Leticia Gomez Rao, Paul S Rennie.   

Abstract

BACKGROUND: We developed non-invasive, cell-based screening assays to rapidly and biologically assess factors that modulate prostate cancer growth and affect androgen receptor (AR) activity.
METHODS: LNCaP cells, which stably express enhanced green fluorescent protein (EGFP) either constitutively or upon AR activation, were treated with a variety of agents, and then monitored by fluorescence and MTS assays for dose-dependent changes in cell number and AR activity.
RESULTS: The assays were validated for rapid, fluorescence-based, quantitative measurement for the presence of growth and AR modulators. Using these assays, we found that osteoblast conditioned media (CM) enhanced prostate cancer cell growth, but not AR activity. After priming with androgen (<1 nM R1881), forskolin or the pesticide dichlorvos enhanced AR activation, whereas interleukin-6 (IL-6) inhibited it.
CONCLUSION: These non-destructive, cell-based assays enable rapid systematic monitoring of the effects of drugs or complex mixtures on prostate cancer cell growth and/or AR activity.

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Year:  2007        PMID: 17219378     DOI: 10.1002/pros.20532

Source DB:  PubMed          Journal:  Prostate        ISSN: 0270-4137            Impact factor:   4.104


  6 in total

1.  Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.

Authors:  Nathan A Lack; Peter Axerio-Cilies; Peyman Tavassoli; Frank Q Han; Ka Hong Chan; Clementine Feau; Eric LeBlanc; Emma Tomlinson Guns; R Kiplin Guy; Paul S Rennie; Artem Cherkasov
Journal:  J Med Chem       Date:  2011-11-18       Impact factor: 7.446

2.  Targeting Binding Function-3 of the Androgen Receptor Blocks Its Co-Chaperone Interactions, Nuclear Translocation, and Activation.

Authors:  Nada Lallous; Eric Leblanc; Ravi S N Munuganti; Mohamed D H Hassona; Nader Al Nakouzi; Shannon Awrey; Helene Morin; Mani Roshan-Moniri; Kriti Singh; Sam Lawn; Takeshi Yamazaki; Hans H Adomat; Christophe Andre; Mads Daugaard; Robert N Young; Emma S Tomlinson Guns; Paul S Rennie; Artem Cherkasov
Journal:  Mol Cancer Ther       Date:  2016-10-07       Impact factor: 6.261

3.  Discovery of novel antagonists targeting the DNA binding domain of androgen receptor by integrated docking-based virtual screening and bioassays.

Authors:  Jin-Ping Pang; Chao Shen; Wen-Fang Zhou; Yun-Xia Wang; Lu-Hu Shan; Xin Chai; Ying Shao; Xue-Ping Hu; Feng Zhu; Dan-Yan Zhu; Li Xiao; Lei Xu; Xiao-Hong Xu; Dan Li; Ting-Jun Hou
Journal:  Acta Pharmacol Sin       Date:  2021-03-25       Impact factor: 7.169

4.  Discovery of Novel Androgen Receptor Ligands by Structure-based Virtual Screening and Bioassays.

Authors:  Wenfang Zhou; Mojie Duan; Weitao Fu; Jinping Pang; Qin Tang; Huiyong Sun; Lei Xu; Shan Chang; Dan Li; Tingjun Hou
Journal:  Genomics Proteomics Bioinformatics       Date:  2019-01-09       Impact factor: 7.691

5.  Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors.

Authors:  Mariia Radaeva; Huifang Li; Eric LeBlanc; Kush Dalal; Fuqiang Ban; Fabrice Ciesielski; Bonny Chow; Helene Morin; Shannon Awrey; Kriti Singh; Paul S Rennie; Nada Lallous; Artem Cherkasov
Journal:  Cells       Date:  2022-09-07       Impact factor: 7.666

6.  Development of Novel Inhibitors Targeting the D-Box of the DNA Binding Domain of Androgen Receptor.

Authors:  Mariia Radaeva; Fuqiang Ban; Fan Zhang; Eric LeBlanc; Nada Lallous; Paul S Rennie; Martin E Gleave; Artem Cherkasov
Journal:  Int J Mol Sci       Date:  2021-03-02       Impact factor: 5.923

  6 in total

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