References

  1. Tsai MJ, O’Malley BW. Molecular mechanisms of action of steroid/thyroid receptor superfamily members. Annu Rev Biochem. 1994;63:451–486.
  2. Evans RM. The steroid and thyroid hormone receptor superfamily. Science. 1988;240:889–895.
  3. Power RF, Conneely OM, O’Malley BW. New insights into activation of the steroid hormone receptor superfamily. Trends Pharmacol Sci. 1992;13:318–323
  4. Mani SK, Allen JM, Lydon JP, Mulac-Jericevic B, Blaustein JD, DeMayo FJ, Conneely O, O’Malley BW. Dopamine requires the unoccupied progesterone receptor to induce sexual behavior in mice. Mol Endocrinol. 1996;10:1728–173
  5. Nazareth LV, Weigel NL. Activation of the human androgen receptor through a protein kinase A signaling pathway. J Biol Chem. 1996;271:19900
  6. Penning TM, Burczynski ME, Jez JM, Hung CF, Lin HK, Ma H, Moore M, Palackal N, Ratnam K. Human 3alpha-hydroxysteroid dehydrogenase isoforms (AKR1C1-AKR1C4) of the aldo-keto reductase superfamily: functional plasticity and tissue distribution reveals roles in the inactivation and formation of male and female sex hormones. Biochem J. 2000;351:67–77.
  7. Imperato-McGinley J, Guerrero L, Gautier T, German JL, Peterson RE. Steroid 5alpha-reductase deficiency in man. An inherited form of male pseudohermaphroditism. Birth Defects Orig Artic Ser. 1975;11:91–103.
  8.  Schindler AE. Metabolism of androstenedione and testosterone in human fetal brain. Prog Brain Res. 1975;42:330.
  9. Liao G, Chen LY, Zhang A, Godavarthy A, Xia F, Ghosh JC, Li H, Chen JD. Regulation of androgen receptor activity by the nuclear receptor corepressor SMRT. J Biol Chem. 2003;278:5052–5061
  10. Shang Y, Myers M, Brown M. Formation of the androgen receptor transcription complex. Mol Cell. 2002;9:601–610.
  11. Hall JM, Couse JF, Korach KS. The multifaceted mechanisms of estradiol and estrogen receptor signaling. J Biol Chem. 2001;276:36869–36872.
  12. Rodan GA, Martin TJ. Therapeutic approaches to bone diseases. Science. 2000;289:1508–1514.
  13.  Dhandapani KM, Brann DW. Protective effects of estrogen and selective estrogen receptor modulators in the brain. Biol Reprod. 2002;67:1379–1385
  14. Burns KA, Korach KS. Estrogen receptors and human disease: an update. Arch Toxicol. 2012;86:1491–1504.
  15. Charles D, Barr W, Bell ET, Brown JB, Fotherby K, Loraine JA. Clomiphene in the Treatment of Oligomenorrhea and Amenorrhea. Am J Obstet Gynecol. 1963;86:913–922.
  16. Kedar RP, Bourne TH, Powles TJ, Collins WP, Ashley SE, Cosgrove DO, Campbell S. Effects of tamoxifen on uterus and ovaries of postmenopausal women in a randomised breast cancer prevention trial. Lancet. 1994;343:1318–1321
  17. Lahti E, Blanco G, Kauppila A, Apaja-Sarkkinen M, Taskinen PJ, Laatikainen T. Endometrial changes in postmenopausal breast cancer patients receiving tamoxifen. Obstet Gynecol. 1993;81:660–664.
  18.  Deligdisch L, Kalir T, Cohen CJ, de Latour M, Le Bouedec G, Penault-Llorca F. Endometrial histopathology in 700 patients treated with tamoxifen for breast cancer. Gynecol Oncol. 2000;78:181–186.
  19. Mincey BA, Moraghan TJ, Perez EA. Prevention and treatment of osteoporosis in women with breast cancer. Mayo Clin Proc. 2000;75:821–829.
  20. Dalton JT, Mukherjee A, Zhu Z, Kirkovsky L, Miller DD. Discovery of nonsteroidal androgens. Biochem Biophys Res Commun. 1998;244:1–4
  21. Link JT, Sorensen B, Patel J, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Wilcox D, Zinker B, Nguyen P, Hickman B, Schmidt JM, Swanson S, Tian Z, Reisch TJ, Rotert G, Du J, Lane B, von Geldern TW, Jacobson PB. Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. J Med Chem. 2005;48:5295–5304.
  22. Tabata Y, Iizuka Y, Shinei R, Kurihara K, Okonogi T, Hoshiko S, Kurata Y. CP8668, a novel orally active nonsteroidal progesterone receptor modulator with tetrahydrobenzindolone skeleton. Eur J Pharmacol. 2003;461:73–78.
  23. Fang S, Suh JM, Reilly SM, Yu E, Osborn O, Lackey D, Yoshihara E, Perino A, Jacinto S, Lukasheva Y, Atkins AR, Khvat A, Schnabl B, Yu RT, Brenner DA, Coulter S, Liddle C, Schoonjans K, Olefsky JM, Saltiel AR, Downes M, Evans RM. Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance. Nat Med. 2015;21:159–165.
  24.  Lubahn DB, Joseph DR, Sar M, Tan J, Higgs HN, Larson RE, French FS, Wilson EM. The human androgen receptor: complementary deoxyribonucleic acid cloning, sequence analysis and gene expression in prostate. Mol Endocrinol. 1988;2:1265–1275. [
  25. Tan JA, Joseph DR, Quarmby VE, Lubahn DB, Sar M, French FS, Wilson EM. The rat androgen receptor: primary structure, autoregulation of its messenger ribonucleic acid, and immunocytochemical localization of the receptor protein. Mol Endocrinol. 1988;2:1276–1285. [
  26. Simental JA, Sar M, Lane MV, French FS, Wilson EM. Transcriptional activation and nuclear targeting signals of the human androgen receptor. J Biol Chem. 1991;266:510–518.
  27. Jenster G, van der Korput HA, Trapman J, Brinkmann AO. Identification of two transcription activation units in the N-terminal domain of the human androgen receptor. J Biol Chem. 1995;270:7341–7346.
  28.  Jenster G, van der Korput HA, van Vroonhoven C, van der Kwast TH, Trapman J, Brinkmann AO. Domains of the human androgen receptor involved in steroid binding, transcriptional activation, and subcellular localization. Mol Endocrinol. 1991;5:1396–1404.
  29. Bevan CL, Hoare S, Claessens F, Heery DM, Parker MG. The AF1 and AF2 domains of the androgen receptor interact with distinct regions of SRC1. Mol Cell Biol. 1999;19:8383–8392.
  30. Alen P, Claessens F, Verhoeven G, Rombauts W, Peeters B. The androgen receptor amino-terminal domain plays a key role in p160 coactivator-stimulated gene transcription. Mol Cell Biol. 1999;19:6085–6095
  31. Ward RD, Weigel NL. Steroid receptor phosphorylation: Assigning function to site-specific phosphorylation. Biofactors. 2009;35:528–530
  32. Kato S, Endoh H, Masuhiro Y, Kitamoto T, Uchiyama S, Sasaki H, Masushige S, Gotoh Y, Nishida E, Kawashima H, Metzger D, Chambon P. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science. 1995;270:1491–1494.
  33. Ylikomi T, Bocquel MT, Berry M, Gronemeyer H, Chambon P. Cooperation of proto-signals for nuclear accumulation of estrogen and progesterone receptors. Embo J. 1992;11:3681–3694
  34. Zhou ZX, Sar M, Simental JA, Lane MV, Wilson EM. A ligand-dependent bipartite nuclear targeting signal in the human androgen receptor. Requirement for the DNA-binding domain and modulation by NH2-terminal and carboxyl-terminal sequences. J Biol Chem. 1994;269:13115–13123.
  35. Mooradian AD, Morley JE, Korenman SG. Biological actions of androgens. Endocr Rev. 1987;8:1–28.
  36.  Holterhus PM, Piefke S, Hiort O. Anabolic steroids, testosterone-precursors and virilizing androgens induce distinct activation profiles of androgen responsive promoter constructs. J Steroid Biochem Mol Biol. 2002;82:269–275.
  37. Permpongkosol S, Khupulsup K, Leelaphiwat S, Pavavattananusorn S, Thongpradit S, Petchthong T. Effects of 8-Year Treatment of Long-Acting Testosterone Undecanoate on Metabolic Parameters, Urinary Symptoms, Bone Mineral Density, and Sexual Function in Men With Late-Onset Hypogonadism. J Sex Med. 2016;13:1199–1211
  38. Traish AM. Testosterone therapy in men with testosterone deficiency: are the benefits and cardiovascular risks real or imagined? Am J Physiol Regul Integr Comp Physiol. 2016;311:R566–573]
  39. Yin D, He Y, Perera MA, Hong SS, Marhefka C, Stourman N, Kirkovsky L, Miller DD, Dalton JT. Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. Mol Pharmacol. 2003;63:211–223
  40. Gao W, Reiser PJ, Coss CC, Phelps MA, Kearbey JD, Miller DD, Dalton JT. Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats. Endocrinology. 2005;146:4887–4897.
  41.  Srinath R, Dobs A. Enobosarm (GTx-024, S-22): a potential treatment for cachexia. Future Oncol. 2014;10:187–194.
  42.  Kearbey JD, Gao W, Narayanan R, Fisher SJ, Wu D, Miller DD, Dalton JT. Selective Androgen Receptor Modulator (SARM) treatment prevents bone loss and reduces body fat in ovariectomized rats. Pharm Res. 2007;24:328–335.
  43.  Crawford J, Prado CM, Johnston MA, Gralla RJ, Taylor RP, Hancock ML, Dalton JT. Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials) Curr Oncol Rep. 2016;18:37.
  44.  Dobs AS, Boccia RV, Croot CC, Gabrail NY, Dalton JT, Hancock ML, Johnston MA, Steiner MS. Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial. Lancet Oncol. 2013;14:335–345.
  45.  Dalton JT, Barnette KG, Bohl CE, Hancock ML, Rodriguez D, Dodson ST, Morton RA, Steiner MS. The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial. J Cachexia Sarcopenia Muscle. 2011;2:153–161.
  46.  Edwards JP, West SJ, Pooley CL, Marschke KB, Farmer LJ, Jones TK. New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone. Bioorg Med Chem Lett. 1998;8:745–750.
  47. Higuchi RI, Edwards JP, Caferro TR, Ringgenberg JD, Kong JW, Hamann LG, Arienti KL, Marschke KB, Davis RL, Farmer LJ, Jones TK. 4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists. Bioorg Med Chem Lett. 1999;9:1335–1340
  48. Miner JN, Chang W, Chapman MS, Finn PD, Hong MH, Lopez FJ, Marschke KB, Rosen J, Schrader W, Turner R, van Oeveren A, Viveros H, Zhi L, Negro-Vilar A. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007;148:363–373.
  49.  Schmidt A, Kimmel DB, Bai C, Scafonas A, Rutledge S, Vogel RL, McElwee-Witmer S, Chen F, Nantermet PV, Kasparcova V, Leu CT, Zhang HZ, Duggan ME, Gentile MA, Hodor P, Pennypacker B, Masarachia P, Opas EE, Adamski SA, Cusick TE, Wang J, Mitchell HJ, Kim Y, Prueksaritanont T, Perkins JJ, Meissner RS, Hartman GD, Freedman LP, Harada S, Ray WJ. 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. J Biol Chem. 2010;285:17054–17064.
  50.  Smith CL, O’Malley BW. Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr Rev. 2004;25:45–71.
  51.  Smith CL, Nawaz Z, O’Malley BW. Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen. Mol Endocrinol. 1997;11:657–666
  52. Madeira M, Mattar A, Logullo AF, Soares FA, Gebrim LH. Estrogen receptor alpha/beta ratio and estrogen receptor beta as predictors of endocrine therapy responsiveness-a randomized neoadjuvant trial comparison between anastrozole and tamoxifen for the treatment of postmenopausal breast cancer. BMC Cancer. 2013;13:425.
  53.  Gao W, Dalton JT. Ockham’s Razor and Selective Androgen Receptor Modulators (SARMs): Are We Overlooking the Role of 5{alpha}-Reductase? Mol Interv. 2007;7:10–13.
  54.  Blouin K, Richard C, Brochu G, Hould FS, Lebel S, Marceau S, Biron S, Luu-The V, Tchernof A. Androgen inactivation and steroid-converting enzyme expression in abdominal adipose tissue in men. J Endocrinol. 2006;191:637–649.
  55.  Labrie F, Luu-The V, Lin SX, Labrie C, Simard J, Breton R, Belanger A. The key role of 17 beta-hydroxysteroid dehydrogenases in sex steroid biology. Steroids. 1997;62:148–158
  56. Penning TM, Byrns MC. Steroid hormone transforming aldo-keto reductases and cancer. Ann N Y Acad Sci. 2009;1155:33–42
  57. Chang CY, McDonnell DP. Androgen receptor-cofactor interactions as targets for new drug discovery. Trends Pharmacol Sci. 2005;26:225–228.
  58.  Heinlein CA, Chang C. Androgen receptor (AR) coregulators: an overview. Endocr Rev. 2002;23:175–200.
  59. Fujimoto N, Yeh S, Kang HY, Inui S, Chang HC, Mizokami A, Chang C. Cloning and characterization of androgen receptor coactivator, ARA55, in human prostate. J Biol Chem. 1999;274:8316–8321
  60. Kang HY, Yeh S, Fujimoto N, Chang C. Cloning and characterization of human prostate coactivator ARA54, a novel protein that associates with the androgen receptor. J Biol Chem. 1999;274:8570–8576
  61. Heery DM, Kalkhoven E, Hoare S, Parker MG. A signature motif in transcriptional co-activators mediates binding to nuclear receptors. Nature. 1997;387:733–736.
  62.  Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell. 1998;95:927–937.
  63.  He B, Minges JT, Lee LW, Wilson EM. The FXXLF motif mediates androgen receptor-specific interactions with coregulators. J Biol Chem. 2002;277:10226–10235.
  64.  Chang CY, McDonnell DP. Evaluation of ligand-dependent changes in AR structure using peptide probes. Mol Endocrinol. 2002;16:647–660.
  65.  Chang C, Norris JD, Gron H, Paige LA, Hamilton PT, Kenan DJ, Fowlkes D, McDonnell DP. Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta. Mol Cell Biol. 1999;19:8226–8239.
  66.  Kazmin D, Prytkova T, Cook CE, Wolfinger R, Chu TM, Beratan D, Norris JD, Chang CY, McDonnell DP. Linking ligand-induced alterations in androgen receptor structure to differential gene expression: a first step in the rational design of selective androgen receptor modulators. Mol Endocrinol. 2006;20:1201–1217
  67. Baek SH, Ohgi KA, Nelson CA, Welsbie D, Chen C, Sawyers CL, Rose DW, Rosenfeld MG. Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells. Proceedings of the National Academy of Sciences of the United States of America. 2006;103:3100–3105
  68. Liu Z, Auboeuf D, Wong J, Chen JD, Tsai SY, Tsai MJ, O’Malley BW. Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486. Proc Natl Acad Sci U S A. 2002;99:7940–7944
  69. Feng Q, O’Malley BW. Nuclear receptor modulation–role of coregulators in selective estrogen receptor modulator (SERM) actions. Steroids. 2014;90:39–43.
  70.  Narayanan R, Yepuru M, Szafran AT, Szwarc M, Bohl CE, Young NL, Miller DD, Mancini MA, Dalton JT. Discovery and mechanistic characterization of a novel selective nuclear androgen receptor exporter for the treatment of prostate cancer. Cancer Res. 2010;70:842–851.
  71.  Guo D, Zhang H, Liu L, Wang L, Cheng Y, Qiao Z. Testosterone influenced the expression of Notch1, Notch2 and Jagged1 induced by lipopolysaccharide in macrophages. Exp Toxicol Pathol. 2004;56:173–179.
  72. Kang HY, Cho CL, Huang KL, Wang JC, Hu YC, Lin HK, Chang C, Huang KE. Nongenomic androgen activation of phosphatidylinositol 3-kinase/Akt signaling pathway in MC3T3-E1 osteoblasts. J Bone Miner Res. 2004;19:1181–1190.
  73. Liu L, Wang L, Zhao Y, Wang Y, Wang Z, Qiao Z. Testosterone attenuates p38 MAPK pathway during Leishmania donovani infection of macrophages. Parasitol Res. 2006;99:189–193.
  74. Huber DM, Bendixen AC, Pathrose P, Srivastava S, Dienger KM, Shevde NK, Pike JW. Androgens suppress osteoclast formation induced by RANKL and macrophage-colony stimulating factor. Endocrinology. 2001;142:3800–3808.
  75. Dehm SM, Tindall DJ. Ligand-independent androgen receptor activity is activation function-2-independent and resistant to antiandrogens in androgen refractory prostate cancer cells. J Biol Chem. 2006;281:27882–27893. [
  76. Kousteni S, Bellido T, Plotkin LI, O’Brien CA, Bodenner DL, Han L, Han K, DiGregorio GB, Katzenellenbogen JA, Katzenellenbogen BS, Roberson PK, Weinstein RS, Jilka RL, Manolagas SC. Nongenotropic, sex-nonspecific signaling through the estrogen or androgen receptors: dissociation from transcriptional activity. Cell. 2001;104:719–730.
  77. Lutz LB, Jamnongjit M, Yang WH, Jahani D, Gill A, Hammes SR. Selective modulation of genomic and nongenomic androgen responses by androgen receptor ligands. Mol Endocrinol. 2003;17:1106–1116.
  78.  Lutz LB, Cole LM, Gupta MK, Kwist KW, Auchus RJ, Hammes SR. Evidence that androgens are the primary steroids produced by Xenopus laevis ovaries and may signal through the classical androgen receptor to promote oocyte maturation. Proc Natl Acad Sci U S A. 2001;98:13728–13733.
  79. Lutz LB, Kim B, Jahani D, Hammes SR. G protein beta gamma subunits inhibit nongenomic progesterone-induced signaling and maturation in Xenopus laevis oocytes. Evidence for a release of inhibition mechanism for cell cycle progression. J Biol Chem. 2000;275:41512–41520.
  80. Narayanan R, Coss CC, Yepuru M, Kearbey JD, Miller DD, Dalton JT. Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways. Mol Endocrinol. 2008;22:2448–2465.
  81. Carmeli E, Coleman R, Reznick AZ. The biochemistry of aging muscle. Exp Gerontol. 2002;37:477–480
  82. Bosy-Westphal A, Eichhorn C, Kutzner D, Illner K, Heller M, Muller MJ. The age-related decline in resting energy expenditure in humans is due to the loss of fat-free mass and to alterations in its metabolically active components. J Nutr. 2003;133:2356–2362.
  83. Muhlberg W, Sieber C. Sarcopenia and frailty in geriatric patients: implications for training and prevention. Z Gerontol Geriatr. 2004;37:2–8.
  84. Wallengren O, Iresjo BM, Lundholm K, Bosaeus I. Loss of muscle mass in the end of life in patients with advanced cancer. Support Care Cancer. 2015;23:79–86.  Liu J, Motoyama S, Sato Y, Wakita A, Kawakita Y, Saito H, Minamiya Y. Decreased Skeletal Muscle Mass After Neoadjuvant Therapy Correlates with Poor Prognosis in Patients with Esophageal Cancer. Anticancer Res. 2016;36:6677–6685.
  85. Chu MP, Lieffers J, Ghosh S, Belch A, Chua NS, Fontaine A, Sangha R, Turner RA, Baracos VE, Sawyer MB. Skeletal muscle density is an independent predictor of diffuse large B-cell lymphoma outcomes treated with rituximab-based chemoimmunotherapy. J Cachexia Sarcopenia Muscle. 2016
  86. van Lierop MJ, Alkema W, Laskewitz AJ, Dijkema R, van der Maaden HM, Smit MJ, Plate R, Conti PG, Jans CG, Timmers CM, van Boeckel CA, Lusher SJ, McGuire R, van Schaik RC, de Vlieg J, Smeets RL, Hofstra CL, Boots AM, van Duin M, Ingelse BA, Schoonen WG, Grefhorst A, van Dijk TH, Kuipers F, Dokter WH. Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index. PLoS One. 2012;7:e48385.
  87. Jones A, Hwang DJ, Narayanan R, Miller DD, Dalton JT. Effects of a novel selective androgen receptor modulator on dexamethasone-induced and hypogonadism-induced muscle atrophy. Endocrinology. 2010;151:3706–3719
  88. Emery AE. Population frequencies of inherited neuromuscular diseases–a world survey. Neuromuscul Disord. 1991;1:19–29.
  89. Rahimov F, Kunkel LM. The cell biology of disease: cellular and molecular mechanisms underlying muscular dystrophy. J Cell Biol. 2013;201:499–510.
  90. Frankel KA, Rosser RJ. The pathology of the heart in progressive muscular dystrophy: epimyocardial fibrosis. Hum Pathol. 1976;7:375–386.
  91. Politano L, Nigro V, Nigro G, Petretta VR, Passamano L, Papparella S, Di Somma S, Comi LI. Development of cardiomyopathy in female carriers of Duchenne and Becker muscular dystrophies. JAMA. 1996;275:1335–1338.
  92. Lim KR, Maruyama R, Yokota T. Eteplirsen in the treatment of Duchenne muscular dystrophy. Drug Des Devel Ther. 2017;11:533–545.
  93.  Cozzoli A, Capogrosso RF, Sblendorio VT, Dinardo MM, Jagerschmidt C, Namour F, Camerino GM, De Luca A. GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy. Pharmacol Res. 2013;72:9–24.
  94.  Ponnusamy S, Sullivan RD, Thiyagarajan T, Tillmann H, Getzenberg RH, Narayanan R. Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice. J Cell Biochem. 2016
  95. Mohler ML, Nair VA, Hwang DJ, Rakov IM, Patil R, Miller DD. Nonsteroidal Tissue Selective Androgen Receptor Modulators: A Promising Class of Clinical Candidates. Expert Opinion in Therapeutic Patents. 2005;15(11):1565–1585.
  96. Hanada K, Furuya K, Yamamoto N, Nejishima H, Ichikawa K, Nakamura T, Miyakawa M, Amano S, Sumita Y, Oguro N. Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat models of osteoporosis. Biol Pharm Bull. 2003;26:1563–1569.
  97.  Hamann LG. Discovery and Preclinical Profile of a Highly Potent and Muscle Selective Androgen Receptor Modulator (SARM). Abstract MEDI 11 from the 227th National American Chemical Society Meeting; Anaheim, CA. March 2004.
  98.  Mason RA, Morris HA. Effects of dihydrotestosterone on bone biochemical markers in sham and oophorectomized rats. J Bone Miner Res. 1997;12:1431–1437.
  99. Coss CC, Jones A, Dalton JT. Selective androgen receptor modulators as improved androgen therapy for advanced breast cancer. Steroids. 2014;90:94–100.
  100. GTx Reports Results from Ongoing Enobosarm Phase 2 Clinical Trial in ER+/AR+ Breast Cancer. 2016
  101. Schwartzberg LS, Yardley D, Elias A, Patel M, LoRusso PM, Burris HA, Gucalp A, Peterson A, Blaney M, Steinberg J, Gibbons J, Traina TA. A Phase I/Ib Study of Enzalutamide Alone and in Combination with Endocrine Therapies in Women with Advanced Breast Cancer. Clin Cancer Res. 2017
  102. Narayanan R, Dalton JT. Androgen Receptor: A Complex Therapeutic Target for Breast Cancer. Cancers (Basel) 2016:8. [
  103. Temel JS, Abernethy AP, Currow DC, Friend J, Duus EM, Yan Y, Fearon KC. Anamorelin in patients with non-small-cell lung cancer and cachexia (ROMANA 1 and ROMANA 2): results from two randomised, double-blind, phase 3 trials. Lancet Oncol. 2016;17:519–531.
  104. Fearon K, Argiles JM, Baracos VE, Bernabei R, Coats A, Crawford J, Deutz NE, Doehner W, Evans WJ, Ferrucci L, Garcia JM, Gralla RJ, Jatoi A, Kalantar-Zadeh K, Lainscak M, Morley JE, Muscaritoli M, Polkey MI, Rosano G, Rossi-Fanelli F, Schols AM, Strasser F, Vellas B, von Haehling S, Anker SD. Request for regulatory guidance for cancer cachexia intervention trials. J Cachexia Sarcopenia Muscle. 2015;6:272–274.
  105. Mohler  ML, Bohl  CE, Jones  A, et al. . Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem. 2009;52:3597–3617.
  106. Dobs  AS, Boccia  RV, Croot  CC, et al. . Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial. Lancet Oncol. 2013;14:335–345.

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