Article
Chaperoning of the A1-adenosine receptor by endogenous adenosine - an extension of the retaliatory metabolite concept.
Molecular pharmacology - 1 Jan 2015
Kusek Justyna, Yang Qiong, Witek Martin, Gruber Christian W, Nanoff Christian, Freissmuth Michael
Abstract excerpt
Cell-permeable orthosteric ligands can assist folding of G protein-coupled receptors in the endoplasmic reticulum (ER); this pharmacochaperoning translates into increased cell surface levels of receptors. Here we used a folding-defective mutant of human A1-adenosine receptor as a sensor to explore whether endogenously produced adenosine can exert a chaperoning effect. This A1-receptor-Y(288)A was retained in the...
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