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The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity

Wifling, David, Bernhardt, Günther, Dove, Stefan and Buschauer, Armin (2015) The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity. PLoS One 10 (1), pp. 1-14.

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Date of publication of this fulltext: 07 Jan 2015 09:55

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Other URL: http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0117185


Abstract

In contrast to the corresponding mouse and rat orthologs, the human histamine H4 receptor (hH4R) shows extraordinarily high constitutive activity. In the extracellular loop, replacement of F169 by V as in the mouse H4R significantly reduced constitutive activity. Stabilization of the inactive state was even more pronounced for a double mutant, in which, in addition to F169V, S179 in the ligand ...

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Item type:Article
Date:28 January 2015
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:Open Access Publizieren (DFG), GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands", GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1371/journal.pone.0117185DOI
25629160PubMed ID
Article ID e0117185Other
Related URLs:
URLURL Type
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0117185Publisher
Keywords:constitutive activity; ligand binding; extracellular loop; ECL2; histamine; histamine H4 receptor; FF motif; site-directed mutagenesis; GTP(gamma)S binding; radioligand binding; Sf9 cells; 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:30927
Owner only: item control page

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