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Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
Guerrero M, Poddutoori R, Urbano M, Peng X, Spicer TP, Chase PS, Hodder PS, Schaeffer MT, Brown S, Rosen H, Roberts E. Guerrero M, et al. Among authors: hodder ps. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6346-9. doi: 10.1016/j.bmcl.2013.09.075. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24135724 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. 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. 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. 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.
98 results