ArticlePloS one2013
Voltage affects the dissociation rate constant of the m2 muscarinic receptor.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 28 citations in OpenAlex.
- Voltage Sensors Embedded in G Protein-Coupled Receptors.International journal of molecular sciences · 2024Review
- Functional consequences of a rare human serotonergic 5-HTFrontiers in pharmacology · 2023Article
- Voltage dependence of the cannabinoid CB1 receptor.Frontiers in pharmacology · 2022Article
- Differential voltage-dependent modulation of the ACh-gated K+ current by adenosine and acetylcholine.PloS one · 2022Article
- Sodium ions allosterically modulate the M2 muscarinic receptor.Scientific reports · 2020Article
- Voltage-Dependent Dopamine Potency at DFrontiers in pharmacology · 2020Article
- G protein-coupled receptors of class A harness the energy of membrane potential to increase their sensitivity and selectivity.Biochimica et biophysica acta. Biomembranes · 2019Article
- Binding kinetics of ligands acting at GPCRs.Molecular and cellular endocrinology · 2019Review
- Interplay between the electrostatic membrane potential and conformational changes in membrane proteins.Protein science : a publication of the Protein Society · 2019Review
- Article
- Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity.Scientific reports · 2017Article
- Emerging concepts in smooth muscle contributions to airway structure and function: implications for health and disease.American journal of physiology. Lung cellular and molecular physiology · 2016Review
- A Novel Voltage Sensor in the Orthosteric Binding Site of the M2 Muscarinic Receptor.Biophysical journal · 2016Article
- Membrane potentials regulating GPCRs: insights from experiments and molecular dynamics simulations.Current opinion in pharmacology · 2016Review
- The agonist-specific voltage dependence of M2 muscarinic receptors modulates the deactivation of the acetylcholine-gated K(+) current (I KACh).Pflugers Archiv : European journal of physiology · 2016Article
- Structural Mechanisms of Voltage Sensing in G Protein-Coupled Receptors.Structure (London, England : 1993) · 2016Article
- Membrane Potential Controls the Efficacy of Catecholamine-induced β1-Adrenoceptor Activity.The Journal of biological chemistry · 2015Article
- Allosteric sodium in class A GPCR signaling.Trends in biochemical sciences · 2014Article
- Thermodynamics of GPCR activation.Biophysics reportsArticle
- Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G-protein coupled receptors (GPCRs) comprise the largest protein family and mediate the vast majority of signal transduction processes in the body. Until recently GPCRs were not considered to be voltage dependent. Newly it was shown for several GPCRs that the first step in GPCR activation, the binding of agonist to the receptor, is voltage sensitive: Voltage shifts the receptor between two states that differ in their binding affinity. Here we show that this shift involves the rate constant of dissociation. We used the m2 muscarinic receptor (m2R) a prototypical GPCR and measured directly the dissociation of [(3)H]ACh from m2R expressed Xenopus oocytes. We show, for the first time, that the voltage dependent change in affinity is implemented by voltage shifting the receptor between two states that differ in their rate constant of dissociation. Furthermore, we provide evidence that suggest that the above shift is achieved by voltage regulating the coupling of the GPCR to its G protein.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.