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Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.
Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Verheij MH, et al. Among authors: nijmeijer s. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5460-4. doi: 10.1016/j.bmcl.2011.06.123. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21782429 Free PMC article.
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
Istyastono EP, Nijmeijer S, Lim HD, van de Stolpe A, Roumen L, Kooistra AJ, Vischer HF, de Esch IJ, Leurs R, de Graaf C. Istyastono EP, et al. Among authors: nijmeijer s. J Med Chem. 2011 Dec 8;54(23):8136-47. doi: 10.1021/jm201042n. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22003888
Molecular pharmacology of histamine H4 receptors.
Nijmeijer S, de Graaf C, Leurs R, Vischer HF. Nijmeijer S, et al. Front Biosci (Landmark Ed). 2012 Jun 1;17(6):2089-106. doi: 10.2741/4039. Front Biosci (Landmark Ed). 2012. PMID: 22652766 Free article. Review.
Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.
Engelhardt H, Schultes S, de Graaf C, Nijmeijer S, Vischer HF, Zuiderveld OP, Dobler J, Stachurski K, Mayer M, Arnhof H, Scharn D, Haaksma EE, de Esch IJ, Leurs R. Engelhardt H, et al. Among authors: nijmeijer s. J Med Chem. 2013 Jun 13;56(11):4264-76. doi: 10.1021/jm301886t. Epub 2013 May 28. J Med Chem. 2013. PMID: 23668417
94 results