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1. Full Text Glucocorticoid Receptor Confers Resistance to Antiandrogens by Bypassing Androgen Receptor Blockade
by Arora, Vivek K and Schenkein, Emily and Murali, Rajmohan and Subudhi, Sumit K and Wongvipat, John and Balbas, Minna D and Shah, Neel and Cai, Ling and Efstathiou, Eleni and Logothetis, Chris and Zheng, Deyou and Sawyers, Charles L
Cell, ISSN 0092-8674, 12/2013, Volume 155, Issue 6, pp. 1309 - 1322
The treatment of advanced prostate cancer has been transformed by novel antiandrogen therapies such as enzalutamide. Here, we identify induction of... 
LUNG-CANCER | GEFITINIB | INHIBITION | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROSTATE-CANCER | MUTATION | GROWTH | INCREASED SURVIVAL | ABIRATERONE | ENZALUTAMIDE | CELL BIOLOGY | Neoplasm Transplantation | Androgen Receptor Antagonists - therapeutic use | Phenylthiohydantoin - therapeutic use | Humans | Receptors, Androgen - metabolism | Gene Expression Regulation | Transcriptome | Drug Resistance, Neoplasm | Male | Receptors, Glucocorticoid - metabolism | Phenylthiohydantoin - analogs & derivatives | Animals | Heterografts | Androgen Antagonists - therapeutic use | Mice | Prostatic Neoplasms - drug therapy | Disease Models, Animal
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2. Full Text Role of the androgen receptor in breast cancer and preclinical analysis of enzalutamide
by Cochrane, Dawn R and Bernales, Sebastián and Jacobsen, Britta M and Cittelly, Diana M and Howe, Erin N and D'Amato, Nicholas C and Spoelstra, Nicole S and Edgerton, Susan M and Jean, Annie and Guerrero, Javier and Gómez, Francisco and Medicherla, Satyanarayana and Alfaro, Iván E and McCullagh, Emma and Jedlicka, Paul and Torkko, Kathleen C and Thor, Ann D and Elias, Anthony D and Protter, Andrew A and Richer, Jennifer K
Breast Cancer Research, ISSN 1465-5411, 01/2014, Volume 16, Issue 1, pp. R7 - R7
Introduction: The androgen receptor (AR) is widely expressed in breast cancers and has been proposed as a therapeutic target in estrogen receptor alpha (ER)... 
ESTROGEN-RECEPTORS | ANTIANDROGEN | ONCOLOGY | TAMOXIFEN | PROSTATE-CANCER | GROWTH | RESISTANCE | NEOADJUVANT ENDOCRINE THERAPY | INHIBITOR | EXPRESSION | CELL-LINE | Neoplasm Transplantation | Anilides - therapeutic use | Androgen Receptor Antagonists - therapeutic use | Phenylthiohydantoin - therapeutic use | Apoptosis - drug effects | Humans | Middle Aged | Receptors, Androgen - metabolism | Transplantation, Heterologous | MCF-7 Cells | Antineoplastic Agents, Hormonal - therapeutic use | Estrogen Receptor alpha - metabolism | Female | Breast Neoplasms - drug therapy | Phenylthiohydantoin - analogs & derivatives | Disease-Free Survival | Animals | Signal Transduction - drug effects | Breast Neoplasms - pathology | Tamoxifen - therapeutic use | Tosyl Compounds - therapeutic use | Androgen Antagonists - therapeutic use | Cell Line, Tumor | Breast Neoplasms - mortality | Cell Proliferation - drug effects | Mice | Nitriles - therapeutic use
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3. Full Text Increased Survival with Enzalutamide in Prostate Cancer after Chemotherapy
by Scher, Howard I and Fizazi, Karim and Saad, Fred and Taplin, Mary-Ellen and Sternberg, Cora N and Miller, Kurt and de Wit, Ronald and Mulders, Peter and Chi, Kim N and Shore, Neal D and Armstrong, Andrew J and Flaig, Thomas W and Fléchon, Aude and Mainwaring, Paul and Fleming, Mark and Hainsworth, John D and Hirmand, Mohammad and Selby, Bryan and Seely, Lynn and de Bono, Johann S and AFFIRM Investigators
The New England Journal of Medicine, ISSN 0028-4793, 09/2012, Volume 367, Issue 13, pp. 1187 - 1197
In a study involving nearly 1200 men with metastatic prostate cancer who had progressive disease after chemotherapy, enzalutamide, a novel androgen-receptor... 
INSTRUMENT | MEDICINE, GENERAL & INTERNAL | THERAPY | ANTIANDROGEN | FUNCTIONAL ASSESSMENT | ANDROGEN-RECEPTOR | CLINICAL-TRIALS | RESISTANCE | MECHANISMS | CARCINOMA | ABIRATERONE | Phenylthiohydantoin - adverse effects | Multivariate Analysis | Androgen Receptor Antagonists - therapeutic use | Double-Blind Method | Phenylthiohydantoin - therapeutic use | Prostatic Neoplasms - surgery | Humans | Middle Aged | Kaplan-Meier Estimate | Male | Antineoplastic Agents - therapeutic use | Androgen Receptor Antagonists - adverse effects | Phenylthiohydantoin - analogs & derivatives | Prostatic Neoplasms - mortality | Orchiectomy | Seizures - chemically induced | Disease-Free Survival | Taxoids - therapeutic use | Neoplasm Metastasis - drug therapy | Signal Transduction - drug effects | Antineoplastic Agents - adverse effects | Aged | Prostatic Neoplasms - drug therapy | Drugs | Dose-response relationship (Biochemistry) | Care and treatment | Product/Service Evaluations | Drug therapy | Prostate cancer | Methods | Cancer | Prostate-specific antigen | Diarrhea | Clinical trials | Fatigue | Survival | Metastases | Testosterone | Signal transduction | Androgens | Chemotherapy | Pain | Castration | Men | Prostate | Seizures
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4. Full Text Conversion of abiraterone to D4A drives anti-tumour activity in prostate cancer
by Li, Zhenfei and Bishop, Andrew C and Alyamani, Mohammad and Garcia, Jorge A and Dreicer, Robert and Bunch, Dustin and Liu, Jiayan and Upadhyay, Sunil K and Auchus, Richard J and Sharifi, Nima
Nature, ISSN 0028-0836, 07/2015, Volume 523, Issue 7560, pp. 347 - 351
Prostate cancer resistance to castration occurs because tumours acquire the metabolic capability of converting precursor steroids to 5... 
ANDROGEN RECEPTOR | 3-BETA-HYDROXYSTEROID DEHYDROGENASE | CYP17A1 INHIBITION | MECHANISM | TESTOSTERONE | RATIONALE | MULTIDISCIPLINARY SCIENCES | INCREASED SURVIVAL | CHEMOTHERAPY | EXPOSURE | ENZALUTAMIDE | Chromatin - metabolism | Prostatic Neoplasms - metabolism | Steroid 17-alpha-Hydroxylase - antagonists & inhibitors | Androgen Receptor Antagonists - therapeutic use | Humans | Receptors, Androgen - metabolism | Gene Expression Regulation, Neoplastic | Androgens - biosynthesis | Male | Androstenes - pharmacology | Androgen Receptor Antagonists - pharmacology | 3-Hydroxysteroid Dehydrogenases - antagonists & inhibitors | Biotransformation | Cell Division | 3-Oxo-5-alpha-Steroid 4-Dehydrogenase - metabolism | 3-Hydroxysteroid Dehydrogenases - metabolism | Prostatic Neoplasms - drug therapy | Dihydrotestosterone - metabolism | Phenylthiohydantoin - pharmacology | Prostatic Neoplasms - pathology | Androstenes - therapeutic use | 5-alpha Reductase Inhibitors - therapeutic use | Prostatic Neoplasms, Castration-Resistant - drug therapy | Phenylthiohydantoin - analogs & derivatives | Androgen Receptor Antagonists - metabolism | Xenograft Model Antitumor Assays | Androstenes - chemistry | Animals | Biosynthetic Pathways - drug effects | Survival Analysis | 5-alpha Reductase Inhibitors - pharmacology | Androstenes - metabolism | Prostatic Neoplasms - enzymology | Mice | Steroid 17-alpha-Hydroxylase - metabolism | 5-alpha Reductase Inhibitors - metabolism | Androgens - metabolism | Enzymes | Testosterone | Androgens | Metabolites | Ligands | Gene expression | Prostate cancer | Tumors
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5. Full Text Enzalutamide in Metastatic Prostate Cancer before Chemotherapy
by Beer, Tomasz M and Armstrong, Andrew J and Rathkopf, Dana E and Loriot, Yohann and Sternberg, Cora N and Higano, Celestia S and Iversen, Peter and Bhattacharya, Suman and Carles, Joan and Chowdhury, Simon and Davis, Ian D and de Bono, Johann S and Evans, Christopher P and Fizazi, Karim and Joshua, Anthony M and Kim, Choung-Soo and Kimura, Go and Mainwaring, Paul and Mansbach, Harry and Miller, Kurt and Noonberg, Sarah B and Perabo, Frank and Phung, De and Saad, Fred and Scher, Howard I and Taplin, Mary-Ellen and Venner, Peter M and Tombal, Bertrand and PREVAIL Investigators
The New England Journal of Medicine, ISSN 0028-4793, 07/2014, Volume 371, Issue 5, pp. 424 - 433
In this study, the androgen-receptor inhibitor enzalutamide improved progression-free and overall survival in men with castration-resistant metastatic prostate... 
MEDICINE, GENERAL & INTERNAL | PREDNISONE | MITOXANTRONE | ANTIANDROGEN | INCREASED SURVIVAL | CASTRATION | ABIRATERONE | Phenylthiohydantoin - adverse effects | Prostatic Neoplasms - pathology | Androgen Receptor Antagonists - therapeutic use | Double-Blind Method | Phenylthiohydantoin - therapeutic use | Administration, Oral | Humans | Male | Neoplasm Metastasis - diagnostic imaging | Adenocarcinoma - drug therapy | Receptors, Androgen | Adenocarcinoma - secondary | Androgen Receptor Antagonists - adverse effects | Disease Progression | Phenylthiohydantoin - analogs & derivatives | Prostatic Neoplasms - mortality | Radiography | Antineoplastic Agents, Hormonal - adverse effects | Antineoplastic Agents, Hormonal - therapeutic use | Survival Analysis | Prostatic Neoplasms - drug therapy | Adenocarcinoma - mortality | Chemotherapy | Care and treatment | Research | Health aspects | Prostate cancer | Cancer | Inhibitor drugs | Castration | Prostate-specific antigen | Cytotoxicity | Fatigue | Metastasis | Survival | Patients | Prostate | Metastases | Life Sciences | Clinical Medicine | Medical and Health Sciences | Cancer and Oncology | Klinisk medicin | Medicin och hälsovetenskap | Cancer och onkologi
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6. Full Text Emerging mechanisms of resistance to androgen receptor inhibitors in prostate cancer
by Watson, Philip A and Arora, Vivek K and Sawyers, Charles L
Nature Reviews Cancer, ISSN 1474-175X, 11/2015, Volume 15, Issue 12, pp. 701 - 711
During the past 10 years, preclinical studies implicating sustained androgen receptor (AR) signalling as the primary driver of castration-resistant prostate... 
MOLECULAR CHARACTERIZATION | SELECTIVE-INHIBITION | POLY(ADP-RIBOSE) POLYMERASE | ONCOLOGY | BRCA MUTATION CARRIERS | SMALL-CELL CARCINOMA | ABIRATERONE ACETATE | PROGESTERONE-RECEPTOR | ANTITUMOR-ACTIVITY | SPLICE VARIANTS | WITHDRAWAL SYNDROME | Androgen Receptor Antagonists - therapeutic use | Animals | Prostatic Neoplasms - genetics | Humans | Drug Resistance, Neoplasm | Male | Gene Expression Regulation, Neoplastic - genetics | Prostatic Neoplasms - drug therapy | Gene mutations | Development and progression | Genetic aspects | Cellular signal transduction | Drug resistance | Prostate cancer | Health aspects | Identification and classification
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7. Full Text Androgen receptor antagonists for prostate cancer therapy
by Helsen, Christine and Van Den Broeck, Thomas and Voet, Arnout and Prekovic, Stefan and Van Poppel, Hendrik and Joniau, Steven and Claessens, Frank
Endocrine-Related Cancer, ISSN 1351-0088, 2014, Volume 21, Issue 4, pp. T105 - T118
Androgen deprivation is the mainstay therapy for metastatic prostate cancer (PCa). Another way of suppressing androgen receptor (AR) signaling is via AR... 
Antiandrogen | Bicalutamide | Androgen receptor antagonist | Enzalutamide | Abiraterone | Prostate cancer | 3 BF3 SITE | MEDROXYPROGESTERONE ACETATE | PHASE-II | LEUPROLIDE ACETATE | bicalutamide | DEPRIVATION THERAPY | prostate cancer | abiraterone | ONCOLOGY | antiandrogen | STRUCTURAL BASIS | ENDOCRINOLOGY & METABOLISM | androgen receptor antagonist | CYPROTERONE-ACETATE | ABIRATERONE ACETATE | LIGAND-BINDING DOMAIN | EUROPEAN-ORGANIZATION | enzalutamide | Prostatic Neoplasms - metabolism | Androgen Receptor Antagonists - therapeutic use | Humans | Receptors, Androgen - metabolism | Male | Antineoplastic Agents - therapeutic use | Androgen Receptor Antagonists - pharmacology | Antineoplastic Agents - chemistry | Animals | Castration | Androgen Receptor Antagonists - chemistry | Antineoplastic Agents - pharmacology | Prostatic Neoplasms - drug therapy
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8. Full Text Phase I Study of ARN-509, a Novel Antiandrogen, in the Treatment of Castration-Resistant Prostate Cancer
by Dana E. Rathkopf and Michael J. Morris and Josef J. Fox and Daniel C. Danila and Susan F. Slovin and Jeffrey H. Hager and Peter J. Rix and Edna Chow Maneval and Isan Chen and Mithat Gönen and Martin Fleisher and Steven M. Larson and Charles L. Sawyers and Howard I. Scher
Journal of Clinical Oncology, ISSN 0732-183X, 10/2013, Volume 31, Issue 28, pp. 3525 - 3530
Purpose ARN-509 is a novel androgen receptor (AR) antagonist for the treatment of castration-resistant prostate cancer (CRPC). ARN-509 inhibits AR nuclear... 
ONCOLOGY | 16-BETA-F-18-FLUORO-5-ALPHA-DIHYDROTESTOSTERONE | INCREASED SURVIVAL | Androgen Antagonists - pharmacokinetics | Androgen Receptor Antagonists - pharmacokinetics | Prostatic Neoplasms - pathology | Androgen Receptor Antagonists - therapeutic use | Prognosis | Follow-Up Studies | Neoplastic Cells, Circulating - pathology | Humans | Middle Aged | Bone Neoplasms - secondary | Male | Prostate-Specific Antigen - blood | Thiohydantoins - pharmacokinetics | Tissue Distribution | Diagnostic Imaging | Maximum Tolerated Dose | Neoplasm Grading | Castration | Thiohydantoins - therapeutic use | Aged, 80 and over | Androgen Antagonists - therapeutic use | Aged | Bone Neoplasms - drug therapy | Prostatic Neoplasms - drug therapy | Index Medicus | Original Reports | Faze
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9. Full Text Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort
by Smith, Matthew R and Antonarakis, Emmanuel S and Ryan, Charles J and Berry, William R and Shore, Neal D and Liu, Glenn and Alumkal, Joshi J and Higano, Celestia S and Chow Maneval, Edna and Bandekar, Rajesh and de Boer, Carla J and Yu, Margaret K and Rathkopf, Dana E
European Urology, ISSN 0302-2838, 2016, Volume 70, Issue 6, pp. 963 - 970
Abstract Background Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation,... 
Urology | Apalutamide | Castration-resistant prostate cancer | Antitumor activity | Safety | DENOSUMAB | CHEMOTHERAPY | Castration-resistant prostate | ANTIANDROGEN | MEN | UROLOGY & NEPHROLOGY | cancer | PLACEBO-CONTROLLED TRIAL | METASTASIS-FREE SURVIVAL | ENZALUTAMIDE | ANTIGEN | Androgen Receptor Antagonists - therapeutic use | Prostatic Neoplasms, Castration-Resistant - blood | Humans | Middle Aged | Male | Treatment Outcome | Prostatic Neoplasms, Castration-Resistant - drug therapy | Prostate-Specific Antigen - blood | Prostatic Neoplasms, Castration-Resistant - pathology | Disease-Free Survival | Neoplasm Grading | Thiohydantoins - therapeutic use | Aged, 80 and over | Aged | Kallikreins - blood | Safety and security measures | Genetic transcription | DNA-ligand interactions | Prostate cancer
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