Cargando…
Sodium ions allosterically modulate the M2 muscarinic receptor
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 musca...
Autores principales: | , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2020
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7341750/ https://www.ncbi.nlm.nih.gov/pubmed/32636499 http://dx.doi.org/10.1038/s41598-020-68133-9 |
Sumario: | 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. |
---|