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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. and Schnell, David and Strasser, Andrea and 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
Subjects: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
Owner: Prof. Dr. Stefan Dove
Deposited On:14 Jun 2010 06:39
Last Modified:14 Jun 2010 06:39
Item ID:15315
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