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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: mcelwee witmer s. 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 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. Among authors: mcelwee witmer s. 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: mcelwee witmer s. 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. Among authors: mcelwee witmer s. 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.
The LATS2/KPM tumor suppressor is a negative regulator of the androgen receptor.
Powzaniuk M, McElwee-Witmer S, Vogel RL, Hayami T, Rutledge SJ, Chen F, Harada S, Schmidt A, Rodan GA, Freedman LP, Bai C. Powzaniuk M, et al. Among authors: mcelwee witmer s. Mol Endocrinol. 2004 Aug;18(8):2011-23. doi: 10.1210/me.2004-0065. Epub 2004 May 6. Mol Endocrinol. 2004. PMID: 15131260