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Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype.
Urbano M, Guerrero M, Velaparthi S, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E. Urbano M, et al. Among authors: hodder p. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6739-45. doi: 10.1016/j.bmcl.2011.09.049. Epub 2011 Sep 20. Bioorg Med Chem Lett. 2011. PMID: 21982495 Free PMC article.
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S. Hale JJ, et al. Among authors: hodder p. J Med Chem. 2004 Dec 30;47(27):6662-5. doi: 10.1021/jm0492507. J Med Chem. 2004. PMID: 15615513
Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II).
Schröter T, Minond D, Weiser A, Dao C, Habel J, Spicer T, Chase P, Baillargeon P, Scampavia L, Schürer S, Chung C, Mader C, Southern M, Tsinoremas N, LoGrasso P, Hodder P. Schröter T, et al. Among authors: hodder p. J Biomol Screen. 2008 Jan;13(1):17-28. doi: 10.1177/1087057107310806. J Biomol Screen. 2008. PMID: 18227223
Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening.
Schürer SC, Brown SJ, Gonzalez-Cabrera PJ, Schaeffer MT, Chapman J, Jo E, Chase P, Spicer T, Hodder P, Rosen H. Schürer SC, et al. Among authors: hodder p. ACS Chem Biol. 2008 Aug 15;3(8):486-98. doi: 10.1021/cb800051m. Epub 2008 Jul 1. ACS Chem Biol. 2008. PMID: 18590333 Free PMC article.
152 results