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Konsta Kukkonen Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland

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Bryn Autio-Kimura Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland

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Hanna Rauhala Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland

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Juha Kesseli Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland

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Matti Nykter Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland
Foundation for the Finnish Cancer Institute, Helsinki, Finland

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Leena Latonen Foundation for the Finnish Cancer Institute, Helsinki, Finland
Institute of Biomedicine, University of Eastern Finland, Kuopio, Finland

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Tapio Visakorpi Faculty of Medicine and Health Technology, Tampere University and Tays Cancer Centre, Tampere University Hospital, Tampere, Finland
Fimlab Laboratories Ltd, Tampere, Finland

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on the gene expression changes related to the activation of AR using our RNA-seq dataset. First, we used unsupervised hierarchical clustering of the HALLMARK ANDROGEN RESPONSE gene set to cluster the cell lines based on their transcriptional response

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Su Jung Oh
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Holger H H Erb
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Alfred Hobisch Division of Experimental Urology, Department of Urology, Department of Urology, Innsbruck Medical University, Anichstrasse 35, A-6020 Innsbruck, Austria

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Frédéric R Santer
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Zoran Culig
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available. Androgen receptor (AR) was shown to play a critical role in progression of prostate cancer ( Grossmann et al . 2001 ). Activated AR interacts with androgen response elements in the promoters of target genes including prostate-specific antigen

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Martina Gruber Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Lavinia Ferrone Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria
Department of Biomedical, Experimental and Clinical Sciences, University of Florence, Florence, Italy

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Martin Puhr Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Frédéric R Santer Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Tobias Furlan Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Iris E Eder Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Natalie Sampson Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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Georg Schäfer Department of Pathology, Neuropathology, and Molecular Pathology, Medical University of Innsbruck, Innsbruck, Austria

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Florian Handle Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria
Molecular Endocrinology Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium

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Zoran Culig Division of Experimental Urology, Department of Urology, Medical University of Innsbruck, Innsbruck, Austria

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dataset GSE77930 ( Kumar et al. 2016 ) was downloaded from the GEO database and analyzed with the Qlucore Omics Explorer v3.5. Gene set activity scores for the Hallmark ‘Androgen response’ and ‘Myc targets’ gene sets (Molecular Signatures Database

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D Alwyn Dart
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Bradley Spencer-Dene Androgen Signalling Laboratory, Department of Histopathology, Department of Oncology, Imperial College London, Du Cane Road, London W12 0NN, UK

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Simon C Gamble
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Jonathan Waxman
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Charlotte L Bevan
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, AR is cytoplasmic; ligand binding induces an active conformation and translocation into the nucleus where it binds specific androgen response elements (AREs) in the regulatory regions of target genes, thus influencing rates of gene transactivation. AR

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Varinder Jeet Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia

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Gregor Tevz Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia

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Melanie Lehman Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia
Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia

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Brett Hollier Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia

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Colleen Nelson Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia
Australian Prostate Cancer Research Centre – Queensland, Department of Urologic Sciences, Institute of Health and Biomedical Innovation, Queensland University of Technology, Princess Alexandra Hospital, Translational Research Institute, Brisbane, Australia

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. 2 A). Furthermore, the androgen-induced increase in YKL40 mRNA was significantly abrogated upon treatment with 10 μM enzalutamide in LNCaP cells, whereas C4-2B cells did not show any significant reduction ( Fig. 2 A). The weak androgen response in

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Charles E Massie Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Inmaculada Spiteri Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Helen Ross-Adams Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Hayley Luxton Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Jonathan Kay Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Hayley C Whitaker Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Mark J Dunning Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Alastair D Lamb Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Antonio Ramos-Montoya Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Daniel S Brewer Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Colin S Cooper Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Rosalind Eeles Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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UK Prostate ICGC Group
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Anne Y Warren Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Simon Tavaré Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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David E Neal Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK
Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Andy G Lynch Cancer Research UK Cambridge Institute, Division of Genetics and Epidemiology, Department of Biological Sciences and School of Medicine, Royal Marsden NHS Foundation Trust, Departments of Pathology, Urology, Surgical Oncology, University of Cambridge, Cambridge, CB2 0RE, UK

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Urano T Ijichi N Ouchi Y Shirahige K Aburatani H 2007 Identification of novel androgen response genes in prostate cancer cells by coupling chromatin immunoprecipitation and genomic microarray analysis . Oncogene 26 4453 – 4463

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Salma Kaochar Department of Medicine, Baylor College of Medicine, Houston, Texas, USA
Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Aleksandra Rusin Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Christopher Foley Department of Medicine, Baylor College of Medicine, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Kimal Rajapakshe Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Matthew Robertson Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Darlene Skapura Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Cammy Mason Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Karen Berman De Ruiz Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Alexey Mikhailovich Tyryshkin Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Jenny Deng Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Jin Na Shin Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Warren Fiskus Department of Medicine, Baylor College of Medicine, Houston, Texas, USA

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Jianrong Dong Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Shixia Huang Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA
Department of Education, Innovation, and Technology, Baylor College of Medicine, Houston, Texas, USA

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Nora M Navone Division of Cancer Medicine, Department of Genitourinary Medical Oncology, The University of Texas Anderson Cancer Center, Houston, Texas, USA

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Christel M Davis Avera Institute for Human Genetics, Sioux Falls, South Dakota, USA

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Erik A Ehli Avera Institute for Human Genetics, Sioux Falls, South Dakota, USA

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Cristian Coarfa Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Nicholas Mitsiades Department of Medicine, Baylor College of Medicine, Houston, Texas, USA
Dan L. Duncan Comprehensive Cancer Center, Houston, Texas, USA
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas, USA

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Korput HA van Eekelen CC van Rooij HC Faber PW Trapman J 1997 An androgen response element in a far upstream enhancer region is essential for high, androgen-regulated activity of the prostate-specific antigen promoter . Molecular Endocrinology

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Philipp Y Maximov Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA

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Balkees Abderrahman Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA

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Ramona F Curpan Institute of Chemistry, Romanian Academy, Timisoara, Romania

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Yousef M Hawsawi Department of Genetics, King Faisal Specialist Hospital & Research Centre, Riyadh, Saudi Arabia

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Ping Fan Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA

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V Craig Jordan Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA

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PSA levels by more than 50% ( Rathkopf et al . 2012 ). The novel small peptide EPI-001 targets the N-terminal domain of the AR containing the activating function-1 region (AF-1). This interrupts the AR’s interaction with other proteins and androgen

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