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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: gentile ma. 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
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. Among authors: gentile ma. 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
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: gentile ma. 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.
Non-invasive muscle contraction assay to study rodent models of sarcopenia.
Chiu CS, Weber H, Adamski S, Rauch A, Gentile MA, Alves SE, Kath G, Flores O, Wilkinson HA. Chiu CS, et al. Among authors: gentile ma. BMC Musculoskelet Disord. 2011 Oct 28;12:246. doi: 10.1186/1471-2474-12-246. BMC Musculoskelet Disord. 2011. PMID: 22035016 Free PMC article.
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: gentile ma. 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: gentile ma. J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r. J Med Chem. 2009. PMID: 19606870
99 results