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Evidence that direct binding of G βγ to the GIRK1 G protein-gated inwardly rectifying K + channel is important for channel activation
Journal article   Open access   Peer reviewed

Evidence that direct binding of G βγ to the GIRK1 G protein-gated inwardly rectifying K + channel is important for channel activation

Chou-Long Huang, Paul A. Slesinger, Patrick J. Casey, Yuh Nung Jan and Lily Y. Jan
Neuron (Cambridge, Mass.), Vol.15(5), pp.1133-1143
1995
DOI: 10.1016/0896-6273(95)90101-9
url
https://doi.org/10.1016/0896-6273(95)90101-9View
Published (Version of record) Open Access

Abstract

Activation of G protein-gated K + channels by G protein-coupled receptors contributes to parasympathetic regulation of heart rate in the atrium and inhibitory postsynaptic potentials in the peripheral and central nervous system. Having found that G βγ activates the cloned GIRK1 channel, we now report evidence for direct binding of G βγ to both the N-terminal hydrophilic domain and amino acids 273–462 of the C-terminal domain of GIRK1. These direct interactions are physiologically important because synthetic peptides derived from either domain reduce the G βγ binding as well as the G βγ activation of the channel. Moreover, the N-terminal domain may also bind trimeric G αβγ, raising the possibility that physical association of G protein-coupled receptors, G proteins, and K + channels partially accounts for their compartmentalization and hence rapid and specific channel activation by receptors.

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