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1. Full Text Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer
by Chris Tran and Samedy Ouk and Nicola J. Clegg and Yu Chen and Philip A. Watson and Vivek Arora and John Wongvipat and Peter M. Smith-Jones and Dongwon Yoo and Andrew Kwon and Teresa Wasielewska and Derek Welsbie and Charlie Degui Chen and Celestia S. Higano and Tomasz M. Beer and David T. Hung and Howard I. Scher and Michael E. Jung and Charles L. Sawyers
Science, ISSN 0036-8075, 5/2009, Volume 324, Issue 5928, pp. 787 - 790
Metastatic prostate cancer is treated with drugs that antagonize androgen action, but most patients progress to a more aggressive form of the disease called... 
COS cells | Androgens | Cell lines | Agonists | Oncology | Reports | Androgen antagonists | Prostate cancer | Heterologous transplantation | Tumors | Vehicles | NONSTEROIDAL ANTIANDROGENS | STRUCTURAL BASIS | AFFINITY | MULTIDISCIPLINARY SCIENCES | ANDROGEN-RECEPTOR | RESISTANCE | ANTAGONISM | LIGAND | MODEL | BICALUTAMIDE | Transcription, Genetic - drug effects | Nitriles - pharmacology | Phenylthiohydantoin - therapeutic use | Humans | Receptors, Androgen - metabolism | Biological Availability | Male | Antineoplastic Agents - therapeutic use | Tosyl Compounds - pharmacology | Antineoplastic Agents - metabolism | Cell Nucleus - metabolism | Receptors, Androgen - chemistry | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Gene Expression Regulation, Neoplastic - drug effects | Prostatic Neoplasms - drug therapy | Androgen Antagonists - pharmacokinetics | Phenylthiohydantoin - pharmacology | Nitriles - metabolism | Prostatic Neoplasms - pathology | Androgen Antagonists - metabolism | Androgen Antagonists - pharmacology | Anilides - metabolism | DNA - metabolism | Phenylthiohydantoin - analogs & derivatives | Xenograft Model Antitumor Assays | Animals | Receptors, Androgen - genetics | Anilides - pharmacology | Tosyl Compounds - metabolism | Androgen Antagonists - therapeutic use | Cell Line, Tumor | Cell Proliferation - drug effects | Mice | Phenylthiohydantoin - metabolism | Drug Screening Assays, Antitumor | Phenylthiohydantoin - pharmacokinetics | Care and treatment | Antiandrogens | Dosage and administration | Drug therapy | Methods | Cancer | Chemotherapy | Pharmacology | Binding sites
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2. Full Text BET bromodomain inhibitors enhance efficacy and disrupt resistance to AR antagonists in the treatment of prostate cancer
by Asangani, Irfan A and Wilder-Romans, Kari and Dommeti, Vijaya L and Krishnamurthy, Pranathi M and Apel, Ingrid J and Escara-Wilke, June and Plymate, Stephen R and Navone, Nora M and Wang, Shaomeng and Feng, Felix Y and Chinnaiyan, Arul M
Molecular Cancer Research, ISSN 1541-7786, 04/2016, Volume 14, Issue 4, pp. 324 - 331
Next-generation antiandrogen therapies, such as enzalutamide and abiraterone, have had a profound impact on the management of metastatic castration-resistant... 
Triazoles - administration & dosage | Antineoplastic Combined Chemotherapy Protocols - administration & dosage | Acetanilides - administration & dosage | Heterocyclic Compounds, 3-Ring - pharmacology | Humans | Receptors, Androgen - metabolism | Male | Androgen Receptor Antagonists - pharmacology | Antineoplastic Combined Chemotherapy Protocols - pharmacology | Phenylthiohydantoin - pharmacology | Cell Survival - drug effects | Acetanilides - pharmacology | Androgen Receptor Antagonists - administration & dosage | Prostatic Neoplasms, Castration-Resistant - drug therapy | Prostatic Neoplasms, Castration-Resistant - metabolism | Phenylthiohydantoin - analogs & derivatives | Azepines - pharmacology | Triazoles - pharmacology | Xenograft Model Antitumor Assays | Phenylthiohydantoin - administration & dosage | Animals | Signal Transduction - drug effects | Heterocyclic Compounds, 3-Ring - administration & dosage | Cell Line, Tumor | Cell Proliferation - drug effects | Mice | Azepines - administration & dosage | Drug Resistance, Neoplasm - drug effects
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3. Full Text The pharmacology of sigma-1 receptors
by Maurice, Tangui and Su, Tsung-Ping
Pharmacology and Therapeutics, ISSN 0163-7258, 2009, Volume 124, Issue 2, pp. 195 - 206
Originally considered an enigmatic protein, the sigma-1 receptor has recently been identified as a unique ligand-regulated molecular chaperone in the... 
Depression | Stroke | Cocaine | Pain | Sigma-1 receptor | Cancer | CONDITIONED PLACE PREFERENCE | NITRIC-OXIDE SYNTHASE | FORCED SWIMMING TEST | HUMAN BREAST-CANCER | INDUCED BEHAVIORAL SENSITIZATION | AMINOTETRAHYDROFURAN DERIVATIVE ANAVEX1-41 | PHARMACOLOGY & PHARMACY | LONG-TERM POTENTIATION | HIPPOCAMPAL CA1 SYNAPSES | TUMOR-CELL-LINES | DORSAL RAPHE NUCLEUS | Behavior, Addictive - drug therapy | Humans | Nervous System Diseases - drug therapy | Analgesics, Opioid - pharmacology | Analgesics, Opioid - therapeutic use | Receptors, sigma - agonists | Receptors, sigma - antagonists & inhibitors | Behavior, Addictive - metabolism | Ion Channel Gating - physiology | Animals | Narcotic Antagonists - therapeutic use | Signal Transduction - drug effects | Narcotic Antagonists - pharmacology | Nervous System Diseases - metabolism | Signal Transduction - physiology | Receptors, sigma - metabolism | Ion Channel Gating - drug effects | Methyl aspartate | Nervous system diseases | Dehydroepiandrosterone | Androgens | Molecular chaperones | Heterocyclic compounds | Depression, Mental | HIV (Viruses) | HIV infection | Alzheimer's disease | pain | cancer | depression | cocaine | stroke
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4. Full Text An F876l mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (Enzalutamide)
by Korpal, Manav and Korn, Joshua M and Gao, Xueliang and Rakiec, Daniel P and Ruddy, David A and Doshi, Shivang and Yuan, Jing and Kovats, Steve G and Kim, Sunkyu and Cooke, Vesselina G and Monahan, John E and Stegmeier, Frank and Roberts, Thomas M and Sellers, William R and Zhou, Wenlai and Zhu, Ping
Cancer Discovery, ISSN 2159-8274, 09/2013, Volume 3, Issue 9, pp. 1030 - 1043
Castration-resistant prostate cancer (CRPC) is the most aggressive, incurable form of prostate cancer. MDV3100 (enzalutamide), an antagonist of the androgen... 
DOMAIN | ONCOLOGY | STATISTICS | ANTIGEN DECLINE | PROSTATE-CANCER | DIRECTED THERAPIES | ANTIANDROGEN WITHDRAWAL SYNDROME | Cyclin-Dependent Kinase 6 - antagonists & inhibitors | Phenylthiohydantoin - pharmacology | Humans | Androgen Antagonists - pharmacology | Male | Prostatic Neoplasms, Castration-Resistant - drug therapy | Androgen Receptor Antagonists - pharmacology | Sequence Analysis, DNA | Phenylthiohydantoin - analogs & derivatives | Drug Resistance, Neoplasm - genetics | Receptors, Androgen - genetics | Base Sequence | Cell Line, Tumor | Mutation | Cyclin-Dependent Kinase 4 - antagonists & inhibitors
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5. Full Text An androgen receptor N-terminal domain antagonist for treating prostate cancer
by Myung, Jae-Kyung and Banuelos, Carmen A and Fernandez, Javier Garcia and Mawji, Nasrin R and Wang, Jun and Tien, Amy H and Yang, Yu Chi and Tavakoli, Iran and Haile, Simon and Watt, Kate and McEwan, Iain J and Plymate, Stephen and Andersen, Raymond J and Sadar, Marianne D
Journal of Clinical Investigation, ISSN 0021-9738, 07/2013, Volume 123, Issue 7, pp. 2948 - 2960
Hormone therapies for advanced prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD), but these ultimately fail and the disease... 
MEDICINE, RESEARCH & EXPERIMENTAL | SIGNAL-TRANSDUCTION PATHWAYS | CELLS | TRANSCRIPTIONAL ACTIVATION | PROTEIN | ANTIANDROGEN | GENE-EXPRESSION | TRANSACTIVATION DOMAIN | TUMOR-GROWTH | PROGRESSION | HORMONE RECEPTORS | Prostatic Neoplasms - metabolism | Stereoisomerism | Humans | Receptors, Androgen - metabolism | Transcriptional Activation - drug effects | Cercopithecus aethiops | Male | Androgen Receptor Antagonists - pharmacology | Benzhydryl Compounds - chemistry | Luciferases - genetics | Androgen Receptor Antagonists - chemistry | Receptors, Androgen - chemistry | Chlorohydrins - pharmacology | Gene Expression Regulation, Neoplastic - drug effects | Genes, Reporter | Prostatic Neoplasms - drug therapy | Protein Structure, Tertiary | Prostatic Neoplasms - pathology | Gene Expression | Antineoplastic Agents, Hormonal - pharmacology | Click Chemistry | Mice, SCID | Chlorohydrins - chemistry | Orchiectomy | Xenograft Model Antitumor Assays | Animals | Receptors, Androgen - genetics | Tumor Burden - drug effects | Protein Binding | Mice, Inbred NOD | Benzhydryl Compounds - pharmacology | Cell Proliferation - drug effects | Mice | Antineoplastic Agents, Hormonal - chemistry | COS Cells | Luciferases - biosynthesis | Antagonists (Biochemistry) | Care and treatment | Androgens | Physiological aspects | Prostate cancer | Health aspects | Methods | Cancer | Proteins | Medical research | Ligands | Kinases | Gene expression | Experiments | Drug dosages | Tumors
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6. 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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7. Full Text Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: A rationale for increasing abiraterone exposure or combining with MDV3100
by Richards, Juliet and Lim, Ai Chiin and Hay, Colin W and Taylor, Angela E and Wingate, Anna and Nowakowska, Karolina and Pezaro, Carmel and Carreira, Suzanne and Goodall, Jane and Arlt, Wiebke and McEwan, Iain J and De Bono, Johann S and Attard, Gerhardt
Cancer Research, ISSN 0008-5472, 05/2012, Volume 72, Issue 9, pp. 2176 - 2182
Prostate cancer progression can be associated with androgen receptor (AR) mutations acquired following treatment with castration and/or an antiandrogen.... 
CELLS | GLUCOCORTICOIDS | CYP17A1 INHIBITION | PHARMACOKINETICS | ANTIANDROGEN | ONCOLOGY | GROWTH | RESISTANT PROSTATE-CANCER | ANTITUMOR-ACTIVITY | ACETATE | I CLINICAL-TRIAL | Binding, Competitive | Phenylthiohydantoin - pharmacology | Prostatic Neoplasms - metabolism | Nitriles - pharmacology | Androstenols - pharmacology | Humans | Receptors, Androgen - metabolism | Androstenes | Male | Androgen Receptor Antagonists - pharmacology | Prednisolone - pharmacology | Phenylthiohydantoin - analogs & derivatives | Tosyl Compounds - pharmacology | Metribolone - metabolism | Drug Interactions | Prostatic Neoplasms - genetics | Receptors, Androgen - genetics | Spironolactone - pharmacology | Androgens - pharmacology | Anilides - pharmacology | Cell Line, Tumor | Spironolactone - antagonists & inhibitors | Spironolactone - analogs & derivatives | Prostatic Neoplasms - drug therapy
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8. Full Text Reciprocal Feedback Regulation of PI3K and Androgen Receptor Signaling in PTEN-Deficient Prostate Cancer
by Carver, Brett S and Chapinski, Caren and Wongvipat, John and Hieronymus, Haley and Chen, Yu and Chandarlapaty, Sarat and Arora, Vivek K and Le, Carl and Koutcher, Jason and Scher, Howard and Scardino, Peter T and Rosen, Neal and Sawyers, Charles L
Cancer Cell, ISSN 1535-6108, 2011, Volume 19, Issue 5, pp. 575 - 586
Prostate cancer is characterized by its dependence on androgen receptor (AR) and frequent activation of PI3K signaling. We find that AR transcriptional output... 
TARGET | CELLS | ONCOLOGY | PATHWAY | DUAL PI3K/MTOR INHIBITOR | KINASE | TUMOR-SUPPRESSOR | AKT | INDUCTION | MTOR COMPLEX | HORMONAL-THERAPY | CELL BIOLOGY | Receptor, ErbB-3 - metabolism | Phosphatidylinositol 3-Kinase - antagonists & inhibitors | Humans | Phosphoprotein Phosphatases - metabolism | Receptors, Androgen - metabolism | Gene Expression Regulation, Neoplastic | Receptor, ErbB-2 - metabolism | Male | Antineoplastic Combined Chemotherapy Protocols - pharmacology | Prostatic Neoplasms - genetics | Receptors, Androgen - drug effects | Transfection | RNA Interference | Time Factors | Transcription, Genetic | Receptor, ErbB-2 - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - metabolism | Phosphatidylinositol 3-Kinase - metabolism | Genes, Reporter | Prostatic Neoplasms - drug therapy | PTEN Phosphohydrolase - genetics | Prostatic Neoplasms - pathology | PTEN Phosphohydrolase - deficiency | Androgen Antagonists - pharmacology | Receptor, ErbB-3 - antagonists & inhibitors | Mice, Transgenic | Nuclear Proteins - metabolism | Mice, SCID | Proto-Oncogene Proteins c-myc - metabolism | Mice, Knockout | Xenograft Model Antitumor Assays | Magnetic Resonance Imaging | Feedback, Physiological | Animals | Signal Transduction - drug effects | Tumor Burden - drug effects | Cell Line, Tumor | Prostatic Neoplasms - enzymology | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Proto-Oncogene Proteins c-myc - genetics | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Phosphatases | Health aspects | Phosphotransferases | Prostate cancer | Analysis | Tumors
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9. Full Text Selective Inhibition of CYP17 With Abiraterone Acetate Is Highly Active in the Treatment of Castration-Resistant Prostate Cancer
by Gerhardt Attard and Alison H.M. Reid and Roger A'Hern and Christopher Parker and Nikhil Babu Oommen and Elizabeth Folkerd and Christina Messiou and L. Rhoda Molife and Gal Maier and Emilda Thompson and David Olmos and Rajesh Sinha and Gloria Lee and Mitch Dowsett and Stan B. Kaye and David Dearnaley and Thian Kheoh and Arturo Molina and Johann S. de Bono
Journal of Clinical Oncology, ISSN 0732-183X, 08/2009, Volume 27, Issue 23, pp. 3742 - 3748
Purpose It has been postulated that castration-resistant prostate cancer (CRPC) commonly remains hormone dependent. Abiraterone acetate is a potent, selective,... 
LEUKEMIA GROUP-B | II CLINICAL-TRIALS | WORKING GROUP | ANTIANDROGEN WITHDRAWAL | ANDROGEN BIOSYNTHESIS | ONCOLOGY | STEROIDAL INHIBITORS | PHASE-II | END-POINTS | DOSE KETOCONAZOLE | HORMONAL-THERAPY | Steroid 17-alpha-Hydroxylase - antagonists & inhibitors | Prospective Studies | Humans | Middle Aged | Drug Resistance, Neoplasm | Male | Neoplasms, Hormone-Dependent - immunology | Androstenols - therapeutic use | Prostatic Neoplasms - immunology | Enzyme Inhibitors - administration & dosage | Antineoplastic Agents, Hormonal - therapeutic use | Aged, 80 and over | Testosterone - blood | Prostatic Neoplasms - drug therapy | Prostatic Neoplasms - pathology | Antineoplastic Agents, Hormonal - pharmacology | Drug Administration Schedule | Androstenols - pharmacology | Antineoplastic Agents, Hormonal - administration & dosage | Enzyme Inhibitors - pharmacology | Kaplan-Meier Estimate | Androgen Antagonists - pharmacology | Androstenes | Enzyme Inhibitors - therapeutic use | Disease Progression | Prostate-Specific Antigen - blood | Neoplasms, Hormone-Dependent - pathology | Androgen Antagonists - therapeutic use | Aged | Androstenols - administration & dosage | Androgen Antagonists - administration & dosage | Neoplasms, Hormone-Dependent - drug therapy | Adrenal Cortex Hormones - administration & dosage
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10. Full Text The impact of sex steroid agonists and antagonists on folliculogenesis in the neonatal porcine ovary via cell proliferation and apoptosis
by Knapczyk-Stwora, Katarzyna and Grzesiak, Malgorzata and Ciereszko, Renata E and Czaja, Elzbieta and Koziorowski, Marek and Slomczynska, Maria
Theriogenology, ISSN 0093-691X, 06/2018, Volume 113, pp. 19 - 26
The objective of the study was to examine the effects of androgen and estrogen agonists or antagonists on the follicle formation, ovarian cell proliferation... 
Endocrine active chemicals | Folliculogenesis | Pig | Steroids | MOUSE | PRIMORDIAL FOLLICLES | FLUTAMIDE | MECHANISMS | OCTYLPHENOL | ESTROGENIC ACTIVITY | IN-VITRO | REPRODUCTIVE BIOLOGY | GROWTH | VETERINARY SCIENCES | EXPRESSION | EXPOSURE | Animals, Newborn | Insecticides - pharmacology | Methoxychlor - pharmacology | Estradiol - analogs & derivatives | Testosterone Propionate - pharmacology | Apoptosis - drug effects | Androgen Antagonists - pharmacology | Flutamide - pharmacology | Estrogen Receptor Antagonists - pharmacology | Ovarian Follicle - drug effects | Animals | Androgens - pharmacology | Swine | Female | Cell Proliferation - drug effects | Granulosa Cells | Estradiol - pharmacology | Phenols - pharmacology | Testosterone | Influenza | Estrogen | Apoptosis
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11. 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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