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Constitutive activity of the human histamine H4 receptor: Molecular modelling, binding and functional studies on wild-type and mutant H4R orthologs

URN to cite this document:
urn:nbn:de:bvb:355-epub-315173
Wifling, David
Date of publication of this fulltext: 30 Mar 2015 13:34


Abstract (English)

The histamine H4R belongs to the class A of G-protein coupled receptors (GPCRs) and is considered as a promising drug target for the treatment of inflammatory diseases such as allergic asthma. The validation of the H4R in translational animal models is compromised by species-dependent differences regarding intrinsic activities, potencies and affinities of ligands, in particular, when comparing ...

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Translation of the abstract (German)

Der Histamin H4R gehört zur Klasse A der G-Protein gekoppelten Rezeptoren (GPCRs) und gilt als vielversprechendes biologisches Zielmolekül für neue Arzneistoffe zur Behandlung von entzündlichen Erkrankungen wie allergischem Asthma. Spezies-abhängige Unterschiede hinsichtlich intrinsischer Aktivitäten, Potenzen und Ligand-Affinitäten limitieren den Vorhersagewert translationaler Tiermodelle für ...

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