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Title:

Interhelical interaction and receptor phosphorylation regulate the activation kinetics of different human ?1-adrenoceptor variants.

Document type:
Journal Article; Article
Author(s):
Ahles, Andrea; Rodewald, Fabian; Rochais, Francesca; Bünemann, Moritz; Engelhardt, Stefan
Abstract:
G protein-coupled receptors represent the largest class of drug targets, but genetic variation within G protein-coupled receptors leads to variable drug responses and, thereby, compromises their therapeutic application. One of the most intensely studied examples is a hyperfunctional variant of the human ?1-adrenoceptor that carries an arginine at position 389 in helix 8 (Arg-389-ADRB1). However, the mechanism underlying the higher efficacy of the Arg-389 variant remained unclear to date. Despite...     »
Journal title abbreviation:
J Biol Chem
Year:
2015
Journal volume:
290
Journal issue:
3
Pages contribution:
1760-9
Language:
eng
Fulltext / DOI:
doi:10.1074/jbc.M114.607333
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/25451930
Print-ISSN:
0021-9258
TUM Institution:
Institut für Pharmakologie und Toxikologie
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