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Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Lim HD, Istyastono EP, van de Stolpe A, Romeo G, Gobbi S, Schepers M, Lahaye R, Menge WM, Zuiderveld OP, Jongejan A, Smits RA, Bakker RA, Haaksma EE, Leurs R, de Esch IJ. Lim HD, et al. Among authors: haaksma ee. Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. doi: 10.1016/j.bmc.2009.04.007. Epub 2009 Apr 11. Bioorg Med Chem. 2009. PMID: 19414267
Linking agonist binding to histamine H1 receptor activation.
Jongejan A, Bruysters M, Ballesteros JA, Haaksma E, Bakker RA, Pardo L, Leurs R. Jongejan A, et al. Among authors: haaksma e. Nat Chem Biol. 2005 Jul;1(2):98-103. doi: 10.1038/nchembio714. Epub 2005 Jun 19. Nat Chem Biol. 2005. PMID: 16408006
Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor.
Nijmeijer S, Engelhardt H, Schultes S, van de Stolpe AC, Lusink V, de Graaf C, Wijtmans M, Haaksma EE, de Esch IJ, Stachurski K, Vischer HF, Leurs R. Nijmeijer S, et al. Among authors: haaksma ee. Br J Pharmacol. 2013 Sep;170(1):89-100. doi: 10.1111/bph.12113. Br J Pharmacol. 2013. PMID: 23347159 Free PMC article.
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: haaksma ee. J Med Chem. 2013 Jun 13;56(11):4264-76. doi: 10.1021/jm301886t. Epub 2013 May 28. J Med Chem. 2013. PMID: 23668417
27 results