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A Potent, Metabolically Stable Tubulin Inhibitor Targets the Colchicine Binding Site and Overcomes Taxane Resistance.

Arnst KE, Wang Y, Hwang DJ, Xue Y, Costello T, Hamilton D, Chen Q, Yang J, Park F, Dalton JT, Miller DD, Li W.

Cancer Res. 2018 Jan 1;78(1):265-277. doi: 10.1158/0008-5472.CAN-17-0577. Epub 2017 Nov 27.


Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer.

Ponnusamy S, Coss CC, Thiyagarajan T, Watts K, Hwang DJ, He Y, Selth LA, McEwan IJ, Duke CB, Pagadala J, Singh G, Wake RW, Ledbetter C, Tilley WD, Moldoveanu T, Dalton JT, Miller DD, Narayanan R.

Cancer Res. 2017 Nov 15;77(22):6282-6298. doi: 10.1158/0008-5472.CAN-17-0976. Epub 2017 Oct 4.


Development of selective androgen receptor modulators (SARMs).

Narayanan R, Coss CC, Dalton JT.

Mol Cell Endocrinol. 2018 Apr 15;465:134-142. doi: 10.1016/j.mce.2017.06.013. Epub 2017 Jun 15. Review.


The long and winding road for selective androgen receptor modulators.

Dalton JT.

Br J Clin Pharmacol. 2017 Oct;83(10):2131-2133. doi: 10.1111/bcp.13345. Epub 2017 Jul 17.


Androgen Receptor: A Complex Therapeutic Target for Breast Cancer.

Narayanan R, Dalton JT.

Cancers (Basel). 2016 Dec 2;8(12). pii: E108. Review.


Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue.

Ponnusamy S, Tran QT, Harvey I, Smallwood HS, Thiyagarajan T, Banerjee S, Johnson DL, Dalton JT, Sullivan RD, Miller DD, Bridges D, Narayanan R.

FASEB J. 2017 Jan;31(1):266-281. doi: 10.1096/fj.201600787RR. Epub 2016 Oct 12.


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).

Crawford J, Prado CM, Johnston MA, Gralla RJ, Taylor RP, Hancock ML, Dalton JT.

Curr Oncol Rep. 2016 Jun;18(6):37. doi: 10.1007/s11912-016-0522-0. Review.


Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin.

Coss CC, Jones A, Dalton JT.

Invest New Drugs. 2016 Aug;34(4):458-67. doi: 10.1007/s10637-016-0353-8. Epub 2016 Apr 22.


Comparison of high-dose intermittent and low-dose continuous oral artemisinin in dogs with naturally occurring tumors.

Hosoya K, Couto CG, London CA, Kisseberth WC, Phelps MA, Dalton JT.

J Am Anim Hosp Assoc. 2014 Nov-Dec;50(6):390-5. doi: 10.5326/JAAHA-MS-6145. Epub 2014 Sep 23.


Design, synthesis, and biological evaluation of stable colchicine binding site tubulin inhibitors as potential anticancer agents.

Lu Y, Chen J, Wang J, Li CM, Ahn S, Barrett CM, Dalton JT, Li W, Miller DD.

J Med Chem. 2014 Sep 11;57(17):7355-66. doi: 10.1021/jm500764v. Epub 2014 Aug 26.


Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling.

Narayanan R, Ahn S, Cheney MD, Yepuru M, Miller DD, Steiner MS, Dalton JT.

PLoS One. 2014 Jul 29;9(7):e103202. doi: 10.1371/journal.pone.0103202. eCollection 2014.


Selective estrogen receptor alpha agonist GTx-758 decreases testosterone with reduced side effects of androgen deprivation therapy in men with advanced prostate cancer.

Yu EY, Getzenberg RH, Coss CC, Gittelman MM, Keane T, Tutrone R, Belkoff L, Given R, Bass J, Chu F, Gambla M, Gaylis F, Bailen J, Hancock ML, Smith J, Dalton JT, Steiner MS.

Eur Urol. 2015 Feb;67(2):334-41. doi: 10.1016/j.eururo.2014.06.011. Epub 2014 Jun 24.


Selective androgen receptor modulators as improved androgen therapy for advanced breast cancer.

Coss CC, Jones A, Dalton JT.

Steroids. 2014 Nov;90:94-100. doi: 10.1016/j.steroids.2014.06.010. Epub 2014 Jun 16. Review.


Selective androgen receptor modulators for the treatment of late onset male hypogonadism.

Coss CC, Jones A, Hancock ML, Steiner MS, Dalton JT.

Asian J Androl. 2014 Mar-Apr;16(2):256-61. doi: 10.4103/1008-682X.122339. Review.


Discovery and preclinical characterization of novel small molecule TRK and ROS1 tyrosine kinase inhibitors for the treatment of cancer and inflammation.

Narayanan R, Yepuru M, Coss CC, Wu Z, Bauler MN, Barrett CM, Mohler ML, Wang Y, Kim J, Snyder LM, He Y, Levy N, Miller DD, Dalton JT.

PLoS One. 2013 Dec 26;8(12):e83380. doi: 10.1371/journal.pone.0083380. eCollection 2013.


TMPRSS2:ERG gene fusion predicts subsequent detection of prostate cancer in patients with high-grade prostatic intraepithelial neoplasia.

Park K, Dalton JT, Narayanan R, Barbieri CE, Hancock ML, Bostwick DG, Steiner MS, Rubin MA.

J Clin Oncol. 2014 Jan 20;32(3):206-11. doi: 10.1200/JCO.2013.49.8386. Epub 2013 Dec 2.


Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer.

Dalton JT, Taylor RP, Mohler ML, Steiner MS.

Curr Opin Support Palliat Care. 2013 Dec;7(4):345-51. doi: 10.1097/SPC.0000000000000015. Review.


Estrogen regulates histone deacetylases to prevent cardiac hypertrophy.

Pedram A, Razandi M, Narayanan R, Dalton JT, McKinsey TA, Levin ER.

Mol Biol Cell. 2013 Dec;24(24):3805-18. doi: 10.1091/mbc.E13-08-0444. Epub 2013 Oct 23.


Effect of para halogen modification of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides on metabolism and clearance.

Kim J, Coss CC, Dalton JT.

Arch Pharm Res. 2014 Nov;37(11):1464-76. doi: 10.1007/s12272-013-0258-4. Epub 2013 Oct 9.


Absorption, distribution, metabolism and excretion of the novel SARM GTx-024 [(S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide] in rats.

Kim J, Wang R, Veverka KA, Dalton JT.

Xenobiotica. 2013 Nov;43(11):993-1009. doi: 10.3109/00498254.2013.788233. Epub 2013 Apr 22.


Steroidogenic enzyme AKR1C3 is a novel androgen receptor-selective coactivator that promotes prostate cancer growth.

Yepuru M, Wu Z, Kulkarni A, Yin F, Barrett CM, Kim J, Steiner MS, Miller DD, Dalton JT, Narayanan R.

Clin Cancer Res. 2013 Oct 15;19(20):5613-25. doi: 10.1158/1078-0432.CCR-13-1151. Epub 2013 Aug 30.


ERβ selective agonist inhibits angiotensin-induced cardiovascular pathology in female mice.

Pedram A, Razandi M, Korach KS, Narayanan R, Dalton JT, Levin ER.

Endocrinology. 2013 Nov;154(11):4352-64. doi: 10.1210/en.2013-1358. Epub 2013 Aug 22.


Standard pentostatin dose reductions in renal insufficiency are not adequate: selected patients with steroid-refractory acute graft-versus-host disease.

Poi MJ, Hofmeister CC, Johnston JS, Edwards RB, Jansak BS, Lucas DM, Farag SS, Dalton JT, Devine SM, Grever MR, Phelps MA.

Clin Pharmacokinet. 2013 Aug;52(8):705-12. doi: 10.1007/s40262-013-0064-7.


Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.

Xiao M, Ahn S, Wang J, Chen J, Miller DD, Dalton JT, Li W.

J Med Chem. 2013 Apr 25;56(8):3318-29. doi: 10.1021/jm4001117. Epub 2013 Apr 9.


Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial.

Dobs AS, Boccia RV, Croot CC, Gabrail NY, Dalton JT, Hancock ML, Johnston MA, Steiner MS.

Lancet Oncol. 2013 Apr;14(4):335-45. doi: 10.1016/S1470-2045(13)70055-X. Epub 2013 Mar 14.


Role of nuclear receptors in lipid dysfunction and obesity-related diseases.

Swanson HI, Wada T, Xie W, Renga B, Zampella A, Distrutti E, Fiorucci S, Kong B, Thomas AM, Guo GL, Narayanan R, Yepuru M, Dalton JT, Chiang JY.

Drug Metab Dispos. 2013 Jan;41(1):1-11. doi: 10.1124/dmd.112.048694. Epub 2012 Oct 4.


Role and pharmacologic significance of cytochrome P-450 2D6 in oxidative metabolism of toremifene and tamoxifen.

Kim J, Coss CC, Barrett CM, Mohler ML, Bohl CE, Li CM, He Y, Veverka KA, Dalton JT.

Int J Cancer. 2013 Mar 15;132(6):1475-85. doi: 10.1002/ijc.27794. Epub 2012 Sep 14.


Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents.

Chen J, Ahn S, Wang J, Lu Y, Dalton JT, Miller DD, Li W.

J Med Chem. 2012 Aug 23;55(16):7285-9. doi: 10.1021/jm300564b. Epub 2012 Aug 6.


Orally bioavailable tubulin antagonists for paclitaxel-refractory cancer.

Li CM, Lu Y, Chen J, Costello TA, Narayanan R, Dalton MN, Snyder LM, Ahn S, Li W, Miller DD, Dalton JT.

Pharm Res. 2012 Nov;29(11):3053-63. doi: 10.1007/s11095-012-0814-5. Epub 2012 Jul 4.


β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization.

Giddabasappa A, Eswaraka JR, Barrett CM, Bauler MN, Wu Z, Yepuru M, Miller DD, Dalton JT.

Invest Ophthalmol Vis Sci. 2012 Jul 31;53(8):5066-75. doi: 10.1167/iovs.12-9627.


Androgen receptor antagonists: a patent review (2008-2011).

Mohler ML, Coss CC, Duke CB 3rd, Patil SA, Miller DD, Dalton JT.

Expert Opin Ther Pat. 2012 May;22(5):541-65. doi: 10.1517/13543776.2012.682571. Review.


Pharmacokinetics, pharmacodynamics and metabolism of a novel anticancer agent for prostate cancer.

Yang J, Ahn S, Wu Z, Hwang DJ, Miller DD, Dalton JT.

Int J Oncol. 2012 Jul;41(1):337-44. doi: 10.3892/ijo.2012.1442. Epub 2012 Apr 20.


Novel tubulin polymerization inhibitors overcome multidrug resistance and reduce melanoma lung metastasis.

Wang Z, Chen J, Wang J, Ahn S, Li CM, Lu Y, Loveless VS, Dalton JT, Miller DD, Li W.

Pharm Res. 2012 Nov;29(11):3040-52. doi: 10.1007/s11095-012-0726-4. Epub 2012 Mar 13.


Preclinical characterization of a novel diphenyl benzamide selective ERα agonist for hormone therapy in prostate cancer.

Coss CC, Jones A, Parke DN, Narayanan R, Barrett CM, Kearbey JD, Veverka KA, Miller DD, Morton RA, Steiner MS, Dalton JT.

Endocrinology. 2012 Mar;153(3):1070-81. doi: 10.1210/en.2011-1608. Epub 2012 Jan 31.


Alanine aminotransferase regulation by androgens in non-hepatic tissues.

Coss CC, Bauler M, Narayanan R, Miller DD, Dalton JT.

Pharm Res. 2012 Apr;29(4):1046-56. doi: 10.1007/s11095-011-0649-5. Epub 2011 Dec 14.


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.

Dalton JT, Barnette KG, Bohl CE, Hancock ML, Rodriguez D, Dodson ST, Morton RA, Steiner MS.

J Cachexia Sarcopenia Muscle. 2011 Sep;2(3):153-161. Epub 2011 Aug 2.


Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization.

Chen J, Li CM, Wang J, Ahn S, Wang Z, Lu Y, Dalton JT, Miller DD, Li W.

Bioorg Med Chem. 2011 Aug 15;19(16):4782-95. doi: 10.1016/j.bmc.2011.06.084. Epub 2011 Jul 1.


Pharmacokinetic optimization of 4-substituted methoxybenzoyl-aryl-thiazole and 2-aryl-4-benzoyl-imidazole for improving oral bioavailability.

Li CM, Chen J, Lu Y, Narayanan R, Parke DN, Li W, Ahn S, Miller DD, Dalton JT.

Drug Metab Dispos. 2011 Oct;39(10):1833-9. doi: 10.1124/dmd.110.036616. Epub 2011 Jul 8.


Drug interaction potential of toremifene and N-desmethyltoremifene with multiple cytochrome P450 isoforms.

Kim J, Peraire C, Solà J, Johanning KM, Dalton JT, Veverka KA.

Xenobiotica. 2011 Oct;41(10):851-62. doi: 10.3109/00498254.2011.590546. Epub 2011 Jul 5.


Mass spectrometric characterization of urinary metabolites of the selective androgen receptor modulator S-22 to identify potential targets for routine doping controls.

Thevis M, Thomas A, Möller I, Geyer H, Dalton JT, Schänzer W.

Rapid Commun Mass Spectrom. 2011 Aug 15;25(15):2187-95. doi: 10.1002/rcm.5100.


Molecular target characterization and antimyeloma activity of the novel, insulin-like growth factor 1 receptor inhibitor, GTx-134.

Liang SB, Yang XZ, Trieu Y, Li Z, Zive J, Leung-Hagesteijn C, Wei E, Zozulya S, Coss CC, Dalton JT, Fantus IG, Trudel S.

Clin Cancer Res. 2011 Jul 15;17(14):4693-704. doi: 10.1158/1078-0432.CCR-10-3097. Epub 2011 Jun 1.


Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.

Lu Y, Li CM, Wang Z, Chen J, Mohler ML, Li W, Dalton JT, Miller DD.

J Med Chem. 2011 Jul 14;54(13):4678-93. doi: 10.1021/jm2003427. Epub 2011 Jun 7.


Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.

Duke CB, Jones A, Bohl CE, Dalton JT, Miller DD.

J Med Chem. 2011 Jun 9;54(11):3973-6. doi: 10.1021/jm2000097. Epub 2011 May 16.


Cancer cachexia therapy: a key weapon in the fight against cancer.

Coss CC, Bohl CE, Dalton JT.

Curr Opin Clin Nutr Metab Care. 2011 May;14(3):268-73. doi: 10.1097/MCO.0b013e3283455e21. Review.


Biotransformation of a novel antimitotic agent, I-387, by mouse, rat, dog, monkey, and human liver microsomes and in vivo pharmacokinetics in mice.

Ahn S, Kearbey JD, Li CM, Duke CB 3rd, Miller DD, Dalton JT.

Drug Metab Dispos. 2011 Apr;39(4):636-43. doi: 10.1124/dmd.110.036673. Epub 2011 Jan 13.


Biological activity of 4-substituted methoxybenzoyl-aryl-thiazole: an active microtubule inhibitor.

Li CM, Wang Z, Lu Y, Ahn S, Narayanan R, Kearbey JD, Parke DN, Li W, Miller DD, Dalton JT.

Cancer Res. 2011 Jan 1;71(1):216-24. doi: 10.1158/0008-5472.CAN-10-1725. Epub 2010 Nov 16.


Flavopiridol pharmacogenetics: clinical and functional evidence for the role of SLCO1B1/OATP1B1 in flavopiridol disposition.

Ni W, Ji J, Dai Z, Papp A, Johnson AJ, Ahn S, Farley KL, Lin TS, Dalton JT, Li X, Jarjoura D, Byrd JC, Sadee W, Grever MR, Phelps MA.

PLoS One. 2010 Nov 1;5(11):e13792. doi: 10.1371/journal.pone.0013792.


MicroRNAs are mediators of androgen action in prostate and muscle.

Narayanan R, Jiang J, Gusev Y, Jones A, Kearbey JD, Miller DD, Schmittgen TD, Dalton JT.

PLoS One. 2010 Oct 27;5(10):e13637. doi: 10.1371/journal.pone.0013637.


Characterization of in vitro generated metabolites of the selective androgen receptor modulators S-22 and S-23 and in vivo comparison to post-administration canine urine specimens.

Thevis M, Gerace E, Thomas A, Beuck S, Geyer H, Schlörer N, Kearbey JD, Dalton JT, Schänzer W.

Drug Test Anal. 2010 Nov-Dec;2(11-12):589-98. doi: 10.1002/dta.211. Epub 2010 Oct 22.


Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.

Chen J, Wang Z, Li CM, Lu Y, Vaddady PK, Meibohm B, Dalton JT, Miller DD, Li W.

J Med Chem. 2010 Oct 28;53(20):7414-27. doi: 10.1021/jm100884b.

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