@inproceedings{349b249707cd46c4a719c601e5b7f744,
title = "Structural Insights into GIRK Channel Function",
abstract = "G protein-gated inwardly rectifying potassium (GIRK; Kir3) channels, which are members of the large family of inwardly rectifying potassium channels (Kir1-Kir7), regulate excitability in the heart and brain. GIRK channels are activated following stimulation of G protein-coupled receptors that couple to the Gi/o (pertussis toxin-sensitive) G proteins. GIRK channels, like all other Kir channels, possess an extrinsic mechanism of inward rectification involving intracellular Mg2+ and polyamines that occlude the conduction pathway at membrane potentials positive to EK. In the past 17 years, more than 20 high-resolution atomic structures containing GIRK channel cytoplasmic domains and transmembrane domains have been solved. These structures have provided valuable insights into the structural determinants of many of the properties common to all inward rectifiers, such as permeation and rectification, as well as revealing the structural bases for GIRK channel gating. In this chapter, we describe advances in our understanding of GIRK channel function based on recent high-resolution atomic structures of inwardly rectifying K+ channels discussed in the context of classical structure-function experiments.",
keywords = "Alcohol, Crystal structure, Electrophysiology, G protein-coupled receptor, G protein-gated inwardly rectifying K channel, Gating, Inhibition, Rectification, X-ray crystallography",
author = "Glaaser, {Ian W.} and Slesinger, {Paul A.}",
note = "Funding Information: We thank Drs. Peter Ung and Avner Schlessinger (Icahn School of Medicine at Mount Sinai) for the GIRK2 model with MPD. Work from the Slesinger lab cited in this chapter was supported by grants from the National Institute on Alcohol Abuse and Alcoholism (AA018734) and the National Institute on Drug Abuse (DA037170; DA025236; DA029706). We apologize to our colleagues whose works could not be included owing to space limitations.",
year = "2015",
doi = "10.1016/bs.irn.2015.05.014",
language = "English",
isbn = "9780128024584",
series = "International Review of Neurobiology",
publisher = "Academic Press Inc.",
pages = "117--160",
editor = "Harris, {R. Adron} and Peter Jenner",
booktitle = "International Review of Neurobiology - Structure to Function of G Protein-Gated Inwardly Rectifying (GIRK) Channels, 2015",
address = "United States",
}