Sodium ions allosterically modulate the M2 muscarinic receptor
| Autor: | Merav Tauber, Yair Ben-Chaim, Sheli Friedman |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Cell biology Sodium Xenopus Allosteric regulation chemistry.chemical_element lcsh:Medicine Biochemistry Article 03 medical and health sciences 0302 clinical medicine Allosteric Regulation Muscarinic acetylcholine receptor Extracellular Animals Receptor lcsh:Science G protein-coupled receptor Receptor Muscarinic M2 Multidisciplinary biology lcsh:R biology.organism_classification Acetylcholine Transmembrane domain 030104 developmental biology chemistry Biophysics lcsh:Q 030217 neurology & neurosurgery Allosteric Site Neuroscience |
| Zdroj: | Scientific Reports Scientific Reports, Vol 10, Iss 1, Pp 1-10 (2020) |
| ISSN: | 2045-2322 |
| Popis: | G protein coupled receptors (GPCRs) play a key role in the vast majority of cellular signal transduction processes. Previous experimental evidence has shown that sodium ion (Na+) allosterically modulate several class A GPCRs and theoretical studies suggested that the same also holds true for muscarinic receptors. Here we examined, using Xenopus oocytes as an expression system, the effect of Na+ on a prototypical GPCR, the M2 muscarinic receptor (M2R). We found that removal of extracellular Na+ resulted in a decrease in the potency of ACh toward the M2R and that a conserved aspartate in transmembrane domain 2 is crucial for this effect. We further show that this allosteric effect of Na+ does not underlie the voltage-dependence of this receptor. |
| Databáze: | OpenAIRE |
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