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Stimulated muscarinic acetylcholine receptors (M2Rs) release Gβγ subunits, which slow heart rate by activating a G protein-gated K+ channel (GIRK). Stimulated β2 adrenergic receptors (β2ARs) also release Gβγ subunits, but GIRK is not activated. This study addresses the mechanism underlying this specificity of GIRK activation by M2Rs. K+ currents and bioluminescence resonance energy transfer between labelled G proteins and GIRK show that M2Rs catalyze Gβγ subunit release at higher rates than β2ARs, generating higher Gβγ concentrations that activate GIRK and regulate other targets of Gβγ. The higher rate of Gβγ release is attributable to a faster G protein coupled receptor - G protein trimer association rate in M2R compared to β2AR. Thus, a rate difference in a single kinetic step accounts for specificity.
Pubmed ID: 30526853 RIS Download
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Software suite for electrophysiology data acquisition and analysis by Molecular Devices. Used for the control and recording of voltage clamp, current clamp, and patch clamp experiments. The software suite consists of Clampex 11 Software for data acquisition, AxoScope 11 Software for background recording, Clampfit 11 Software for data analysis, and optional Clampfit Advanced Analysis Module for sophisticated and streamlined analysis.
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View all literature mentionsCell line tsA201 is a Transformed cell line with a species of origin Homo sapiens
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View all literature mentionsCell line Flp-In-T-REx-293 is a Transformed cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line CHO is a Spontaneously immortalized cell line with a species of origin Cricetulus griseus (Chinese hamster)
View all literature mentionsCell line Sf9 is a Spontaneously immortalized cell line with a species of origin Spodoptera frugiperda
View all literature mentionsA technical computing software and computing environment that provides users with algorithms and mathematical functions for various projects and purposes. The resource incorporates other Wolfram products such as Wolfram Algorithmbase, Wolfram Language, and Wolfram Knowledgebase.
View all literature mentionsCell line tsA201 is a Transformed cell line with a species of origin Homo sapiens
View all literature mentionsCell line Flp-In-T-REx-293 is a Transformed cell line with a species of origin Homo sapiens (Human)
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