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Updated: Jan 4, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
The coupling of the M2 muscarinic receptor to its G protein is voltage dependent
Yair Ben-Chaim1, Chava Broide2, Hanna Parnas2
1Department of Natural and Life Sciences, The Open University of Israel, Ra'anana, Israel.
Abstract:
G protein coupled receptors (GPCRs) participate in the majority of signal transduction processes in the body. Specifically, the binding of an external agonist promotes coupling of the GPCR to its G protein and this, in turn, induces downstream signaling. Recently, it was shown that agonist binding to the M2 muscarinic receptor (M2R) and to other GPCRs is voltage dependent. Here we examine, whether the coupling of the M2R to its G protein is also voltage-dependent. We first show, in Xenopus oocytes, that the activity of the M2R in the absence of agonist (constitutive activity) can be used to report the coupling. We then show that the coupling is, by itself, voltage dependent. This novel finding is of physiological importance, as it shows that the actual signal transduction, whose first step is the coupling of the GPCR to its cognate G protein, is voltage dependent.
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