Sodium ions allosterically modulate the M2 muscarinic receptor

Sheli Friedman, Merav Tauber, Yair Ben-Chaim

نتاج البحث: نشر في مجلةمقالةمراجعة النظراء


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.

اللغة الأصليةالإنجليزيّة
رقم المقال11177
دوريةScientific Reports
مستوى الصوت10
رقم الإصدار1
المعرِّفات الرقمية للأشياء
حالة النشرنُشِر - 1 ديسمبر 2020

ملاحظة ببليوغرافية

Funding Information:
This work was supported by an internal Grant from the Open University of Israel.

Publisher Copyright:
© 2020, The Author(s).


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