Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 983.36 of the human histamine H4 receptor
British Journal of Pharmacology2013Vol. 170(1), pp. 89–100
Citations Over TimeTop 17% of 2013 papers
Saskia Nijmeijer, Harald Engelhardt, Sabine Schultes, Andrea C. van de Stolpe, V Lusink, Chris de Graaf, Maikel Wijtmans, Eric Haaksma, Iwan J. P. de Esch, Katharina Stachurski, Henry F. Vischer, Rob Leurs
Abstract
VUF14480 is thought to bind covalently to the hH₄ receptor-C98(3.36) residue and partially induce hH₄ receptor-mediated G protein activation and β-arrestin2 recruitment. Moreover, these observations confirm our previously proposed binding mode of 2-aminopyrimidines. VUF14480 will be a useful tool to stabilize the receptor into an active confirmation and further investigate the structure of the active hH₄ receptor.
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