@article{7e72c4331a1c4b28bb2e920544ea52d2,
title = "Evidence that direct binding of Gβγ to the GIRK1 G protein-gated inwardly rectifying K+ channel is important for channel activation",
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 Gβγ activates the cloned GIRK1 channel, we now report evidence for direct binding of Gβγ 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 Gβγ binding as well as the Gβγ activation of the channel. Moreover, the N-terminal domain may also bind trimeric Gαβγ, 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.",
author = "Huang, {Chou Long} and Slesinger, {Paul A.} and Casey, {Patrick J.} and Jan, {Yuh Nung} and Jan, {Lily Y.}",
note = "Funding Information: All correspondence should be addressed to L. Y. J. We thank Y. J. Liao for purifying IRK1 and GIRK1 antibodies; C. Turck for synthesizing the peptides; A. G. Gilman, S. M. Mumby, and P. C. Sternweis for anti-G~., antibodies and G~,~-expressing baculoviruses; D. Clapham for CIRcDNA; H. Bourne, A. Collins, H.-H. Chuang, Y. J. Liao, M. Sheng, A. Tinker, and J. Yang for comments on the manuscript; and L. Acker-man, S. Barbel, and W. Walantus for art work. This work was supported by the California Affiliate of the American Heart Association Postdoctoral Fellowship (C.-L. H.), a grant from the American Cancer Society (P. J. C.), and a National Institute of Mental Health grant to the Silvio Conte Center for Neuroscience at the University of California, San Francisco. P. A. S. is a Howard Hughes Medical Institute Associate. Y. N. J. and L. Y. J. are Howard Hughes Investigators. The costs of publication of this article were defrayed in part by the payment of page charges. This article must therefore be hereby marked {"}advertisement{"} in accordance with 18 USC Section 1734 solely to indicate this fact.",
year = "1995",
month = nov,
doi = "10.1016/0896-6273(95)90101-9",
language = "English (US)",
volume = "15",
pages = "1133--1143",
journal = "Neuron",
issn = "0896-6273",
publisher = "Cell Press",
number = "5",
}