Pharmacochaperoning of the ER-retained A1 adenosine receptor

Selective Inhibitory Effect of Adenosine A1 Receptor Agonists on the Proliferation of Human Tumor Cell Lines

Background: In this study, the effects of three structural analogues of adenosine upon proliferation of human tumor cells were investigated. Previous research showed a cytotoxic effect of adenosine via A3 receptor and A1 receptor and sometimes this effect was receptor independent. The researches showed a differential cytotoxic effect of adenosine and its A3 agonists on cancerous cells, while ot...

PET imaging of adenosine A1 receptor occupancy.

Anxiolytic properties of A1 adenosine receptor PAMs

Anxiety and anxiety disorders are among the most prevalent mental health conditions worldwide. Despite the high prevalence rates, anxiety is often an underestimated and undertreated clinical problem. Current treatment strategy for the management of anxiety mainly involves the use of selective serotonin reuptake inhibitors and benzodiazepines. Although widely prescribed and effective in reducing...

Chaperoning of the A1-adenosine receptor by endogenous adenosine - an extension of the retaliatory metabolite concept.

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 w...

Chaperoning of the A1-Adenosine Receptor by Endogenous Adenosine—An Extension of the Retaliatory Metabolite Concept s

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 A was ...