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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: rosen h. 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.
Sphingosine 1-phosphate receptor signaling.
Rosen H, Gonzalez-Cabrera PJ, Sanna MG, Brown S. Rosen H, et al. Annu Rev Biochem. 2009;78:743-68. doi: 10.1146/annurev.biochem.78.072407.103733. Annu Rev Biochem. 2009. PMID: 19231986 Review.
Actions of a picomolar short-acting S1P₁ agonist in S1P₁-eGFP knock-in mice.
Cahalan SM, Gonzalez-Cabrera PJ, Sarkisyan G, Nguyen N, Schaeffer MT, Huang L, Yeager A, Clemons B, Scott F, Rosen H. Cahalan SM, et al. Among authors: rosen h. Nat Chem Biol. 2011 May;7(5):254-6. doi: 10.1038/nchembio.547. Epub 2011 Mar 27. Nat Chem Biol. 2011. PMID: 21445057 Free PMC article.
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: rosen h. 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.
Novel selective allosteric and bitopic ligands for the S1P(3) receptor.
Jo E, Bhhatarai B, Repetto E, Guerrero M, Riley S, Brown SJ, Kohno Y, Roberts E, Schürer SC, Rosen H. Jo E, et al. Among authors: rosen h. ACS Chem Biol. 2012 Dec 21;7(12):1975-83. doi: 10.1021/cb300392z. Epub 2012 Sep 14. ACS Chem Biol. 2012. PMID: 22971058 Free PMC article.
1,893 results