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Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.
Harcken C, Riether D, Kuzmich D, Liu P, Betageri R, Ralph M, Emmanuel M, Reeves JT, Berry A, Souza D, Nelson RM, Kukulka A, Fadra TN, Zuvela-Jelaska L, Dinallo R, Bentzien J, Nabozny GH, Thomson DS. Harcken C, et al. Among authors: souza d. J Med Chem. 2014 Feb 27;57(4):1583-98. doi: 10.1021/jm4019178. Epub 2014 Feb 7. J Med Chem. 2014. PMID: 24506830
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
Regan J, Lee TW, Zindell RM, Bekkali Y, Bentzien J, Gilmore T, Hammach A, Kirrane TM, Kukulka AJ, Kuzmich D, Nelson RM, Proudfoot JR, Ralph M, Pelletier J, Souza D, Zuvela-Jelaska L, Nabozny G, Thomson DS. Regan J, et al. Among authors: souza d. J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t. J Med Chem. 2006. PMID: 17181172
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.
Betageri R, Gilmore T, Kuzmich D, Kirrane TM, Bentzien J, Wiedenmayer D, Bekkali Y, Regan J, Berry A, Latli B, Kukulka AJ, Fadra TN, Nelson RM, Goldrick S, Zuvela-Jelaska L, Souza D, Pelletier J, Dinallo R, Panzenbeck M, Torcellini C, Lee H, Pack E, Harcken C, Nabozny G, Thomson DS. Betageri R, et al. Among authors: souza d. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6842-51. doi: 10.1016/j.bmcl.2011.09.018. Epub 2011 Sep 10. Bioorg Med Chem Lett. 2011. PMID: 21963986
The oxidase activity of vascular adhesion protein-1 (VAP-1) is essential for function.
Noonan T, Lukas S, Peet GW, Pelletier J, Panzenbeck M, Hanidu A, Mazurek S, Wasti R, Rybina I, Roma T, Kronkaitis A, Shoultz A, Souza D, Jiang H, Nabozny G, Modis LK. Noonan T, et al. Among authors: souza d. Am J Clin Exp Immunol. 2013 Jun 15;2(2):172-85. Print 2013. Am J Clin Exp Immunol. 2013. PMID: 23885334 Free PMC article.
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.
Razavi H, Riether D, Harcken C, Bentzien J, Dinallo RM, Souza D, Nelson RM, Kukulka A, Fadra-Khan TN, Pack EJ Jr, Zuvela-Jelaska L, Pelletier J, Panzenbeck M, Torcellini CA, Proudfoot JR, Nabozny GH, Thomson DS. Razavi H, et al. Among authors: souza d. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1934-40. doi: 10.1016/j.bmcl.2014.03.005. Epub 2014 Mar 12. Bioorg Med Chem Lett. 2014. PMID: 24656565
A GPBAR1 (TGR5) small molecule agonist shows specific inhibitory effects on myeloid cell activation in vitro and reduces experimental autoimmune encephalitis (EAE) in vivo.
Lewis ND, Patnaude LA, Pelletier J, Souza DJ, Lukas SM, King FJ, Hill JD, Stefanopoulos DE, Ryan K, Desai S, Skow D, Kauschke SG, Broermann A, Kuzmich D, Harcken C, Hickey ER, Modis LK. Lewis ND, et al. Among authors: souza dj. PLoS One. 2014 Jun 26;9(6):e100883. doi: 10.1371/journal.pone.0100883. eCollection 2014. PLoS One. 2014. PMID: 24967665 Free PMC article.
Kcnn4 is a regulator of macrophage multinucleation in bone homeostasis and inflammatory disease.
Kang H, Kerloc'h A, Rotival M, Xu X, Zhang Q, D'Souza Z, Kim M, Scholz JC, Ko JH, Srivastava PK, Genzen JR, Cui W, Aitman TJ, Game L, Melvin JE, Hanidu A, Dimock J, Zheng J, Souza D, Behera AK, Nabozny G, Cook HT, Bassett JH, Williams GR, Li J, Vignery A, Petretto E, Behmoaras J. Kang H, et al. Among authors: souza d, d souza z. Cell Rep. 2014 Aug 21;8(4):1210-24. doi: 10.1016/j.celrep.2014.07.032. Epub 2014 Aug 14. Cell Rep. 2014. PMID: 25131209 Free PMC article.
3,659 results