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Impact of the DRY Motif and the Missing "Ionic Lock" on Constitutive Activity and G-Protein Coupling of the Human Histamine H-4 Receptor

Schneider, Erich H., Schnell, David, Strasser, Andrea, Dove, Stefan and Seifert, Roland (2010) Impact of the DRY Motif and the Missing "Ionic Lock" on Constitutive Activity and G-Protein Coupling of the Human Histamine H-4 Receptor. Journal of Pharmacology and Experimental Therapeutics 333 (2), pp. 382-392.

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Abstract

It is assumed that many G protein-coupled receptors (GPCRs) are restrained in an inactive state by the "ionic lock," an interaction between an arginine in transmembrane domain (TM) 3 (R3.50) and a negatively charged residue in TM6 (D/E6.30). In the human histamine H-4 receptor (hH(4)R), alanine is present in position 6.30. To elucidate whether this mutation causes the high constitutive activity ...

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Item type:Article
Date:2010
Additional Information (public):584UE Times Cited:1 Cited References Count:40
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
ISI:000276777900004Other
DOI 10.1124/jpet.109.163220Other
Keywords:a(2a) adenosine receptor crystal-structure amino-acid beta(2)-adrenergic receptor structural instability adrenergic-receptor guinea-pig activation rhodopsin state
Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:15315
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