Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H(4) receptor

BACKGROUND AND PURPOSE: The recently proposed binding mode of 2-aminopyrimidines to the human (h) histamine H(4) receptor suggests that the 2-amino group of these ligands interacts with glutamic acid residue E182(5.46) in the transmembrane (TM) helix 5 of this receptor. Interestingly, substituents a...

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Hlavní autoři: Nijmeijer, S, Engelhardt, H, Schultes, S, van de Stolpe, A C, Lusink, V, de Graaf, C, Wijtmans, M, Haaksma, E E J, de Esch, I J P, Stachurski, K, Vischer, H F, Leurs, R
Médium: Artigo
Jazyk:Inglês
Vydáno: Blackwell Publishing Ltd 2013
Témata:
Themed Issue: Histamine Pharmacology Update
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC3764852/
https://ncbi.nlm.nih.gov/pubmed/23347159
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1111/bph.12113
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