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Modulation of GPCRs by monovalent cations and anions

Strasser, Andrea ; Wittmann, Hans-Joachim ; Schneider, Erich H. ; Seifert, Roland


The recent resolution of G-protein-coupled receptor (GPCR) structures in complex with Na+ bound to an allosteric modulatory site has renewed interest of the regulation of GPCRs by ions. Here, we summarise key data on ion modulation of GPCRs, obtained in pharmacological, crystallographic, mutagenesis and molecular modelling studies. We show that ion modulation is a highly complex process, ...


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