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The preclinical efficacy, selectivity and pharmacologic profile of MK-5932, an insulin-sparing selective glucocorticoid receptor modulator.
Brandish PE, Anderson K, Baltus GA, Bai C, Bungard CJ, Bunting P, Byford A, Chiu CS, Cicmil M, Corcoran H, Euler D, Fisher JE, Gambone C, Hasbun-Manning M, Kuklin N, Landis E, Lifsted TQ, McElwee-Witmer S, McIntosh IS, Meissner RS, Miao J, Mitchell HJ, Musselman A, Schmidt A, Shin J, Szczerba P, Thompson CD, Tribouley C, Vogel RL, Warrier S, Hershey JC. Brandish PE, et al. Among authors: schmidt a. Eur J Pharmacol. 2014 Feb 5;724:102-11. doi: 10.1016/j.ejphar.2013.12.031. Epub 2013 Dec 27. Eur J Pharmacol. 2014. PMID: 24374007
Discovery of selective glucocorticoid receptor modulator MK-5932.
Bungard CJ, Hartman GD, Manikowski JJ, Perkins JJ, Bai C, Brandish PE, Euler DH, Hershey JC, Schmidt A, Fang Y, Norcross RT, Rushmore TH, Thompson CD, Meissner RS. Bungard CJ, et al. Among authors: schmidt a. Bioorg Med Chem. 2011 Dec 15;19(24):7374-86. doi: 10.1016/j.bmc.2011.10.054. Epub 2011 Oct 24. Bioorg Med Chem. 2011. PMID: 22079253
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.
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. Schmidt A, et al. J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31. J Biol Chem. 2010. PMID: 20356837 Free PMC article.
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Mitchell HJ, Dankulich WP, Hartman GD, Prueksaritanont T, Schmidt A, Vogel RL, Bai C, McElwee-Witmer S, Zhang HZ, Chen F, Leu CT, Kimmel DB, Ray WJ, Nantermet P, Gentile MA, Duggan ME, Meissner RS. Mitchell HJ, et al. Among authors: schmidt a. J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r. J Med Chem. 2009. PMID: 19606870
Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.
Schmidt A, Harada SI, Kimmel DB, Bai C, Chen F, Rutledge SJ, Vogel RL, Scafonas A, Gentile MA, Nantermet PV, McElwee-Witmer S, Pennypacker B, Masarachia P, Sahoo SP, Kim Y, Meissner RS, Hartman GD, Duggan ME, Rodan GA, Towler DA, Ray WJ. Schmidt A, et al. J Biol Chem. 2009 Dec 25;284(52):36367-36376. doi: 10.1074/jbc.M109.049734. Epub 2009 Oct 21. J Biol Chem. 2009. PMID: 19846549 Free PMC article.
Identification of an anabolic selective androgen receptor modulator that actively induces death of androgen-independent prostate cancer cells.
Schmidt A, Meissner RS, Gentile MA, Chisamore MJ, Opas EE, Scafonas A, Cusick TE, Gambone C, Pennypacker B, Hodor P, Perkins JJ, Bai C, Ferraro D, Bettoun DJ, Wilkinson HA, Alves SE, Flores O, Ray WJ. Schmidt A, et al. J Steroid Biochem Mol Biol. 2014 Sep;143:29-39. doi: 10.1016/j.jsbmb.2014.02.005. Epub 2014 Feb 22. J Steroid Biochem Mol Biol. 2014. PMID: 24565564
A novel selective androgen receptor modulator (SARM) MK-4541 exerts anti-androgenic activity in the prostate cancer xenograft R-3327G and anabolic activity on skeletal muscle mass & function in castrated mice.
Chisamore MJ, Gentile MA, Dillon GM, Baran M, Gambone C, Riley S, Schmidt A, Flores O, Wilkinson H, Alves SE. Chisamore MJ, et al. Among authors: schmidt a. J Steroid Biochem Mol Biol. 2016 Oct;163:88-97. doi: 10.1016/j.jsbmb.2016.04.007. Epub 2016 Apr 19. J Steroid Biochem Mol Biol. 2016. PMID: 27106747
6,611 results