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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

Wifling, David (2015) Constitutive activity of the human histamine H4 receptor: Molecular modelling, binding and functional studies on wild-type and mutant H4R orthologs. PhD, Universität Regensburg.

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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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Item type:Thesis of the University of Regensburg (PhD)
Date:30 March 2015
Referee:Prof. Dr. Armin Buschauer
Date of exam:13 March 2015
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Keywords:constitutive activity, Sf9 cells, ligand binding, H4 receptor, H4 receptor orthologs, histamine, site-directed mutagenesis, GTP(gamma)S binding, radioligand binding, JNJ7777120, clozapine, isoloxapine, VUF8430, immepip, clobenpropit, thioperamide, UR-PI376, UR-PI294
Dewey Decimal Classification:600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:31517
Owner only: item control page

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