Delineation of Agonist Binding to the Human Histamine H4 Receptor Using Mutational Analysis, Homology Modeling, and ab Initio Calculations

@article{Jongejan2008DelineationOA,
  title={Delineation of Agonist Binding to the Human Histamine H4 Receptor Using Mutational Analysis, Homology Modeling, and ab Initio Calculations},
  author={Aldo Jongejan and Herman D. Lim and Rogier A. Smits and Iwan J. P. de Esch and Eric E. J. Haaksma and Rob Leurs},
  journal={Journal of chemical information and modeling},
  year={2008},
  volume={48 7},
  pages={1455-63}
}
A three-dimensional homology model of the human histamine H 4 receptor was developed to investigate the binding mode of a series of structurally diverse H 4-agonists, i.e. histamine, clozapine, and the recently described selective, nonimidazole agonist VUF 8430. Mutagenesis studies and docking of these ligands in a rhodopsin-based homology model revealed two essential points of interactions in the binding pocket, i.e. Asp3.32 and Glu5.46 (Ballesteros-Weinstein numbering system). It is… CONTINUE READING

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