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Ninu Poulose
Ninu Poulose
Centre for Cancer Research and Cell Biology, Queen’s University of Belfast, Belfast, UK
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Ian G Mills
Ian G Mills
Centre for Cancer Research and Cell Biology, Queen’s University of Belfast, Belfast, UK
Nuffield Department of Surgical Sciences, John Radcliffe Hospital, University of Oxford, Oxford, UK
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Nuffield Department of Surgical Sciences, John Radcliffe Hospital, University of Oxford, Oxford, UK
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Rebecca E Steele
Rebecca E Steele
Centre for Cancer Research and Cell Biology, Queen’s University of Belfast, Belfast, UK
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and binding to androgen response elements in the promoter regions of target genes, such as prostate-specific antigen (PSA) and transmembrane protease serine 2 ( Tan et al . 2015 ). AR is expressed mostly in the secretory epithelial cells and to some
Douglas A Gibson
Douglas A Gibson
MRC Centre for Reproductive Health The University of Edinburgh, The Queen's Medical Research Institute, 47 Little France Crescent, Edinburgh EH16 4TJ, UK
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Ioannis Simitsidellis
Ioannis Simitsidellis
MRC Centre for Reproductive Health The University of Edinburgh, The Queen's Medical Research Institute, 47 Little France Crescent, Edinburgh EH16 4TJ, UK
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Frances Collins
Frances Collins
MRC Centre for Reproductive Health The University of Edinburgh, The Queen's Medical Research Institute, 47 Little France Crescent, Edinburgh EH16 4TJ, UK
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Philippa T K Saunders
Philippa T K Saunders
MRC Centre for Reproductive Health The University of Edinburgh, The Queen's Medical Research Institute, 47 Little France Crescent, Edinburgh EH16 4TJ, UK
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F Maggiolini M 2010 Inhibition of cyclin D1 expression by androgen receptor in breast cancer cells – identification of a novel androgen response element . Nucleic Acids Research 38 5351 – 5365 . ( doi:10.1093/nar/gkq278 ). Lepine J
Kathryn E Ware
Kathryn E Ware
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Mariano A Garcia-Blanco
Mariano A Garcia-Blanco
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Andrew J Armstrong
Andrew J Armstrong
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Scott M Dehm
Scott M Dehm
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
Departments of Molecular Genetics and Medicine Duke University, 213 Research Dr, 0045 CARL Building, Durham, North Carolina 27710, USA
Department of Medicine Duke Cancer Institute, Duke University, Durham, North Carolina, USA
Masonic Cancer Center University of Minnesota Masonic Cancer Center, Mayo Mail Code 806, 420 Delaware Street SE, Minneapolis, Minnesota 55455, USA
Department of Laboratory Medicine and Pathology University of Minnesota, Minneapolis, Minnesota, USA
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recognizing and binding androgen-response elements (AREs) in the promoters and enhancers of AR transcriptional targets. When bound to DNA, the AR NTD accounts for the majority of AR transcriptional activity through interactions with co-regulators. Figure 1 AR
Muhammed H Rahaman
Muhammed H Rahaman
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Malika Kumarasiri
Malika Kumarasiri
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Laychiluh B Mekonnen
Laychiluh B Mekonnen
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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Mingfeng Yu
Mingfeng Yu
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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Sarah Diab
Sarah Diab
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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Hugo Albrecht
Hugo Albrecht
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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Robert W Milne
Robert W Milne
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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Shudong Wang
Shudong Wang
Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia
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acids 101–360) and TAU5 (amino acids 370–494) ( Jenster et al. 1995 ). In contrast, DBD is highly conserved and contains two zinc fingers; one binds to a specific nucleotide, the androgen response element (ARE), and the other promotes homodimerization
Fazlul H Sarkar
Fazlul H Sarkar
Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, 740 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
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Yiwei Li
Yiwei Li
Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, 740 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
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Zhiwei Wang
Zhiwei Wang
Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, 740 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
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Dejuan Kong
Dejuan Kong
Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, 740 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
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nuclear compartment, AR homodimer formation, and its interaction with DNA ( Heinlein & Chang 2002 , 2004 ). The activated AR then initiates gene transcription by binding to specific androgen response elements in the promoter regions of target genes ( Fig
Isabel Coutinho
Isabel Coutinho
Dame Roma Mitchell Cancer Research Laboratories, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Tanya K Day
Tanya K Day
Dame Roma Mitchell Cancer Research Laboratories, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Wayne D Tilley
Wayne D Tilley
Dame Roma Mitchell Cancer Research Laboratories, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Luke A Selth
Luke A Selth
Dame Roma Mitchell Cancer Research Laboratories, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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Freemasons Foundation Centre for Men’s Health, School of Medicine, The University of Adelaide, Adelaide, South Australia, Australia
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inverted repeat androgen response elements ( Chan et al . 2015 ). Second, dimerization of AR-Vs is required for their transcriptional activity and utilizes the same interaction surface as AR-FL ( Chan et al . 2015 , Xu et al . 2015 ). Finally
Keely M McNamara
Keely M McNamara
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Nicole L Moore
Nicole L Moore
Department of Pathology Tohoku University School of Medicine, Miyagi, Sendai, Japan
Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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Theresa E Hickey
Theresa E Hickey
Department of Pathology Tohoku University School of Medicine, Miyagi, Sendai, Japan
Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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Hironobu Sasano
Hironobu Sasano
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Wayne D Tilley
Wayne D Tilley
Department of Pathology Tohoku University School of Medicine, Miyagi, Sendai, Japan
Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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Dame Roma Mitchell Cancer Research Laboratories Discipline of Medicine, The University of Adelaide and Hanson Institute, DX 650801, Adelaide, South Australia 5005, Australia
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F Maggiolini M 2010 Inhibition of cyclin D1 expression by androgen receptor in breast cancer cells – identification of a novel androgen response element . Nucleic Acids Research 38 5351 – 5365 . ( doi:10.1093/nar/gkq278 ). Lanzino M
Shyh-Han Tan
Shyh-Han Tan
Department of Cancer Biology, Kimmel Cancer Center, Thomas Jefferson University, 233 South 10th Street, BLSB 309, Philadelphia, Pennsylvania 19107, USA
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Marja T Nevalainen
Marja T Nevalainen
Department of Cancer Biology, Kimmel Cancer Center, Thomas Jefferson University, 233 South 10th Street, BLSB 309, Philadelphia, Pennsylvania 19107, USA
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receptor (AR) induces the dissociation from heat shock proteins (HSPs), receptor phosphorylation, and dimerization. Dimerized AR is translocated into the nucleus and bind to androgen response elements at the promoter of target genes. In prostate cancer
Philipp Y Maximov
Philipp Y Maximov
Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA
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Balkees Abderrahman
Balkees Abderrahman
Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA
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Ramona F Curpan
Ramona F Curpan
Institute of Chemistry, Romanian Academy, Timisoara, Romania
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Yousef M Hawsawi
Yousef M Hawsawi
Department of Genetics, King Faisal Specialist Hospital & Research Centre, Riyadh, Saudi Arabia
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Ping Fan
Ping Fan
Department of Breast Medical Oncology, MD Anderson Cancer Centre, Houston, Texas, USA
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V Craig Jordan
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
D M Peehl
D M Peehl
Department of Urology, Stanford University School of Medicine, Stanford, California, USA
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cell cytokeratins, and other differentiation markers such as PSA remain low ( Peehl et al. 1994 b , Goosens et al. 2002). Continuous exposure to collagenase was reported to retain androgen response ( Mitchen et al. 1997 ), but this methodology has
