Strasser, Andrea and Wittmann, Hans-Joachim and Schneider, Erich H. and Seifert, Roland (2015) Modulation of GPCRs by monovalent cations and anions. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 388 (3). pp. 363-380. ISSN 0028-1298, 1432-1912
Full text not available from this repository. (Request a copy)Abstract
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, involving not only cations but also, rather neglected until now, anions. Pharmacotherapeutic and toxicological aspects are discussed. We provide a mathematical framework for the analysis of ion effects. Finally, we discuss open questions in the field and future research directions. Most importantly, the in vivo relevance of the modulation of GPCR function by monovalent ions must be clarified.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ALPHA2-ADRENERGIC RECEPTOR SYSTEM; BINDING REGULATORY PROTEINS; HIGH CONSTITUTIVE ACTIVITY; ALKALI-METAL IONS; SODIUM-IONS; CANNABINOID RECEPTORS; ALLOSTERIC MODULATION; ANTAGONIST BINDING; DOPAMINE-RECEPTORS; OPIOID RECEPTORS; GPCR; Monovalent cations; Monovalent anions; Modelling; Pharmacology |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Petra Gürster |
| Date Deposited: | 14 Aug 2020 09:29 |
| Last Modified: | 14 Aug 2020 09:29 |
| URI: | https://pred.uni-regensburg.de/id/eprint/5921 |
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