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Review

Therapeutic potential of the SARMs: revisiting the androgen receptor for drug discovery

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Pages 377-387 | Published online: 21 Mar 2006

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Eva de Rijke, Martien L. Essers, Jeroen C.W. Rijk, Mario Thevis, Toine F.H. Bovee, Leendert A. van Ginkel & Saskia S. Sterk. (2013) Selective androgen receptor modulators: in vitro and in vivo metabolism and analysis. Food Additives & Contaminants: Part A 30:9, pages 1517-1526.
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Michael L Mohler, Ramesh Narayanan, Christopher C Coss, Kejiang Hu, Yali He, Zhongzhi Wu, Seoung-Soo Hong, Dong Jin Hwang, Duane D Miller & James T Dalton. (2010) Estrogen receptor β selective nonsteroidal estrogens: seeking clinical indications. Expert Opinion on Therapeutic Patents 20:4, pages 507-534.
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Xuqing Zhang, James C Lanter & Zhihua Sui. (2009) Recent advances in the development of selective androgen receptor modulators. Expert Opinion on Therapeutic Patents 19:9, pages 1239-1258.
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Gordon S Lynch. (2008) Update on emerging drugs for sarcopenia – age-related muscle wasting. Expert Opinion on Emerging Drugs 13:4, pages 655-673.
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Emily Pfeil & Adrian S Dobs. (2008) Current and future testosterone delivery systems for treatment of the hypogonadal male. Expert Opinion on Drug Delivery 5:4, pages 471-481.
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Daniel Edelstein, Mala Sivanandy, Sadeka Shahani & Shehzad Basaria. (2007) The latest options and future agents for treating male hypogonadism. Expert Opinion on Pharmacotherapy 8:17, pages 2991-3008.
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Daniel Edelstein, Adrian Dobs & Shehzad Basaria. (2006) Emerging drugs for hypogonadism. Expert Opinion on Emerging Drugs 11:4, pages 685-707.
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K. O. Böker, M. Komrakova, L. Fahrendorff, B. R. Spelsberg, D. B. Hoffmann, A. F. Schilling, W. Lehmann, S. Taudien & S. Sehmisch. (2023) Treatment of osteoporosis using a selective androgen receptor modulator ostarine in an orchiectomized rat model. Endocrine 81:3, pages 579-591.
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A. Kaufmann, A. Arrizabalaga-Larrañaga, M.H. Blokland & S.S. Sterk. (2023) Potential and limitation of retrospective HRMS based data analysis: “Have meat-producing animals been exposed to illegal growth promotors such as SARMs?”. Food Control 147, pages 109611.
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Marina Komrakova, Judith Furtwängler, Daniel Bernd Hoffmann, Wolfgang Lehmann, Arndt Friedrich Schilling & Stephan Sehmisch. (2019) The Selective Androgen Receptor Modulator Ostarine Improves Bone Healing in Ovariectomized Rats. Calcified Tissue International 106:2, pages 147-157.
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Emiliano Ventura, Anna Gadaj, Gail Monteith, Alexis Ripoche, Jim Healy, Francesco Botrè, Saskia S. Sterk, Tom Buckley & Mark H. Mooney. (2019) Development and validation of a semi-quantitative ultra-high performance liquid chromatography-tandem mass spectrometry method for screening of selective androgen receptor modulators in urine. Journal of Chromatography A 1600, pages 183-196.
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Peter Y. Liu & Johannes D. Veldhuis. 2019. Yen and Jaffe's Reproductive Endocrinology. Yen and Jaffe's Reproductive Endocrinology 285 300.e8 .
Stephan Haehling. (2017) Wasting away: How to treat cachexia and muscle wasting in chronic disease?. British Journal of Clinical Pharmacology 83:12, pages 2599-2601.
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Kyle J. Hackney, Jessica M. Scott, Andrea M. Hanson, Kirk L. English, Meghan E. Downs & Lori L. Ploutz-Snyder. (2015) The Astronaut-Athlete. Journal of Strength and Conditioning Research 29:12, pages 3531-3545.
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Steven Karch & Olaf Drummer. 2015. Karch's Pathology of Drug Abuse, Fifth Edition. Karch's Pathology of Drug Abuse, Fifth Edition 755 784 .
Peter Y. Liu & Johannes D. Veldhuis. 2014. Yen & Jaffe's Reproductive Endocrinology. Yen & Jaffe's Reproductive Endocrinology 272 286.e8 .
Heinrich Burkhardt. 2013. Drug Therapy for the Elderly. Drug Therapy for the Elderly 303 309 .
Christopher C. Coss, Matt Bauler, Ramesh Narayanan, Duane D. Miller & James T. Dalton. (2011) Alanine Aminotransferase Regulation by Androgens in Non-hepatic Tissues. Pharmaceutical Research 29:4, pages 1046-1056.
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Shayne Cox GadGregory T. Wurz & Michael W. DeGregorio. 2010. Pharmaceutical Sciences Encyclopedia. Pharmaceutical Sciences Encyclopedia.
Dimitrios D. Nikolopoulos, Chara Spiliopoulou & Stamatios E. Theocharis. (2011) Doping and musculoskeletal system: short-term and long-lasting effects of doping agents. Fundamental & Clinical Pharmacology 25:5, pages 535-563.
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Shontelle DodsonVickie E. BaracosAminah JatoiWilliam J. EvansDavid CellaJames T. DaltonMitchell S. Steiner. (2011) Muscle Wasting in Cancer Cachexia: Clinical Implications, Diagnosis, and Emerging Treatment Strategies. Annual Review of Medicine 62:1, pages 265-279.
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Azriel Schmidt, Donald B. Kimmel, Chang Bai, Angela Scafonas, SuJane Rutledge, Robert L. Vogel, Sheila McElwee-Witmer, Fang Chen, Pascale V. Nantermet, Viera Kasparcova, Chih-tai Leu, Hai-Zhuan Zhang, Mark E. Duggan, Michael A. Gentile, Paul Hodor, Brenda Pennypacker, Patricia Masarachia, Evan E. Opas, Sharon A. Adamski, Tara E. Cusick, Jiabing Wang, Helen J. Mitchell, Yuntae Kim, Thomayant Prueksaritanont, James J. Perkins, Robert S. Meissner, George D. Hartman, Leonard P. Freedman, Shun-ichi Harada & William J. Ray. (2010) Discovery of the Selective Androgen Receptor Modulator MK-0773 Using a Rational Development Strategy Based on Differential Transcriptional Requirements for Androgenic Anabolism Versus Reproductive Physiology. Journal of Biological Chemistry 285:22, pages 17054-17064.
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Roberta Diaz Brinton. 2010. Brocklehurst's Textbook of Geriatric Medicine and Gerontology. Brocklehurst's Textbook of Geriatric Medicine and Gerontology 163 169 .
Kirk J. Brower. 2011. Addiction Medicine. Addiction Medicine 533 549 .
Robert M. Johnston, Linda N. Chu, Mark Liu, Steven L. Goldberg, Animesh Goswami & Ramesh N. Patel. (2009) Hydroxylation of l-proline to cis-3-hydroxy-l-proline by recombinant Escherichia coli expressing a synthetic l-proline-3-hydroxylase gene. Enzyme and Microbial Technology 45:6-7, pages 484-490.
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Mihail F Zilbermint & Adrian S Dobs. (2009) Nonsteroidal selective androgen receptor modulator Ostarine ™ in cancer cachexia . Future Oncology 5:8, pages 1211-1220.
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Jay R Hoffman, William J Kraemer, Shalender Bhasin, Thomas Storer, Nicholas A Ratamess, G Gregory Haff, Darryn S Willoughby & Alan D Rogol. (2009) Position Stand on Androgen and Human Growth Hormone Use. Journal of Strength and Conditioning Research 23:Supplement 5, pages S1-S59.
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Michael L. Mohler, Casey E. Bohl, Amanda Jones, Christopher C. Coss, Ramesh Narayanan, Yali He, Dong Jin Hwang, James T. Dalton & Duane D. Miller. (2009) Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit. Journal of Medicinal Chemistry 52:12, pages 3597-3617.
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Peter Y. Liu & Johannes D. Veldhuis. 2009. Yen & Jaffe's Reproductive Endocrinology. Yen & Jaffe's Reproductive Endocrinology 283 298 .
Michael L. Mohler, Casey E. Bohl, Ramesh Narayanan, Yali He, Dong Jin Hwang, James T. Dalton & Duane D. Miller. 2008. Nuclear Receptors as Drug Targets. Nuclear Receptors as Drug Targets 249 304 .
G N Brooke, M G Parker & C L Bevan. (2007) Mechanisms of androgen receptor activation in advanced prostate cancer: differential co-activator recruitment and gene expression. Oncogene 27:21, pages 2941-2950.
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RLYKA DRESNER-POLLAK, S. AUBREY STOCH & MICHAEL ROSENBLATT. 2008. Osteoporosis. Osteoporosis 1837 1895 .
Xuqing Zhang, Xiaojie Li, George F. Allan, Tifanie Sbriscia, Olivia Linton, Scott G. Lundeen & Zhihua Sui. (2007) Design, Synthesis, and in Vivo SAR of a Novel Series of Pyrazolines as Potent Selective Androgen Receptor Modulators. Journal of Medicinal Chemistry 50:16, pages 3857-3869.
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Monty Montano, John N. Flanagan, Lan Jiang, Paola Sebastiani, Matthew Rarick, Nathan K. LeBrasseur, Carl A. Morris, Ravi Jasuja & Shalender Bhasin. (2007) Transcriptional Profiling of Testosterone-Regulated Genes in the Skeletal Muscle of Human Immunodeficiency Virus-Infected Men Experiencing Weight Loss. The Journal of Clinical Endocrinology & Metabolism 92:7, pages 2793-2802.
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Lawrence G. Hamann, Mark C. Manfredi, Chongqing Sun, Stanley R. KrystekJr.Jr., Yanting Huang, Yingzhi Bi, David J. Augeri, Tammy Wang, Yan Zou, David. A. Betebenner, Aberra Fura, Ramakrishna Seethala, Rajasree Golla, Joyce E. Kuhns, John A. Lupisella, Celia J. Darienzo, Laura L. Custer, Jennifer L. Price, James M. Johnson, Scott A. Biller, Robert Zahler & Jacek Ostrowski. (2007) Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators. Bioorganic & Medicinal Chemistry Letters 17:7, pages 1860-1864.
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Gordon S. Lynch, Jonathan D. Schertzer & James G. Ryall. (2007) Therapeutic approaches for muscle wasting disorders. Pharmacology & Therapeutics 113:3, pages 461-487.
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Wenqing Gao & James T. Dalton. (2007) Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs). Drug Discovery Today 12:5-6, pages 241-248.
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Raymond A. Ng, James C. Lanter, Vernon C. Alford, George F. Allan, Tifanie Sbriscia, Scott G. Lundeen & Zhihua Sui. (2007) Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold. Bioorganic & Medicinal Chemistry Letters 17:6, pages 1784-1787.
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