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Page 1
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Brown AR, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, Elmore MA, Firth A, Goodwin R, Goutcher S, Grant E, Grassie M, Grove SJ, Hamilton NM, Hampson H, Hillier A, Ho KK, Kiczun M, Kingsbury C, Kultgen SG, Littlewood PT, Lusher SJ, Macdonald S, McIntosh L, McIntyre T, Mistry A, Morphy JR, Nimz O, Ohlmeyer M, Pick J, Rankovic Z, Sherborne B, Smith A, Speake M, Spinks G, Thomson F, Watson L, Weston M. Brown AR, et al. Among authors: lusher sj. Bioorg Med Chem Lett. 2011 Jan 1;21(1):137-40. doi: 10.1016/j.bmcl.2010.11.054. Epub 2010 Nov 16. Bioorg Med Chem Lett. 2011. PMID: 21129964
Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.
van Lierop MJ, Alkema W, Laskewitz AJ, Dijkema R, van der Maaden HM, Smit MJ, Plate R, Conti PG, Jans CG, Timmers CM, van Boeckel CA, Lusher SJ, McGuire R, van Schaik RC, de Vlieg J, Smeets RL, Hofstra CL, Boots AM, van Duin M, Ingelse BA, Schoonen WG, Grefhorst A, van Dijk TH, Kuipers F, Dokter WH. van Lierop MJ, et al. Among authors: lusher sj. PLoS One. 2012;7(11):e48385. doi: 10.1371/journal.pone.0048385. Epub 2012 Nov 12. PLoS One. 2012. PMID: 23152771 Free PMC article.
X-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11β-substituted steroids.
Lusher SJ, Raaijmakers HC, Vu-Pham D, Kazemier B, Bosch R, McGuire R, Azevedo R, Hamersma H, Dechering K, Oubrie A, van Duin M, de Vlieg J. Lusher SJ, et al. J Biol Chem. 2012 Jun 8;287(24):20333-43. doi: 10.1074/jbc.M111.308403. Epub 2012 Apr 25. J Biol Chem. 2012. PMID: 22535964 Free PMC article.
Data-driven medicinal chemistry in the era of big data.
Lusher SJ, McGuire R, van Schaik RC, Nicholson CD, de Vlieg J. Lusher SJ, et al. Drug Discov Today. 2014 Jul;19(7):859-68. doi: 10.1016/j.drudis.2013.12.004. Epub 2013 Dec 17. Drug Discov Today. 2014. PMID: 24361338 Review.
14 results