G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity

G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels are mainly expressed in excitable cells such as neurons and atrial myocytes, where they can respond to a wide variety of neurotransmitters. Four GIRK subunits have been found in mammals (GIRK1-4) and act as downstream targets for various Ga...

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Autores: Martín Belmonte, Alejandro, Aguado Rubio, Carolina, Alfaro Ruiz, Rocío, Luján Miras, Rafael
Formato: artículo
Fecha de publicación:2025
País:España
Recursos:Universidad de Castilla-La Mancha
Repositorio:RUIdeRA. Repositorio Institucional de la UCLM
OAI Identifier:oai:ruidera.uclm.es:10578/42854
Acesso em linha:https://www.hh.um.es/Abstracts/Vol_/_/__18822.htm
https://hdl.handle.net/10578/42854
Access Level:acceso abierto
Palavra-chave:G protein-coupled receptors (GPCRs)
GIRK channels
Hyperpolarization
Immunoelectron microscopy
Immunohistochemistry
Inhibition
Macromolecular complexes
Neurological diseases
Neurons
Pathology
Pharmacological targets
Potassium efflux
Subcellular localization
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spelling G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversityMartín Belmonte, AlejandroAguado Rubio, CarolinaAlfaro Ruiz, RocíoLuján Miras, RafaelG protein-coupled receptors (GPCRs)GIRK channelsHyperpolarizationImmunoelectron microscopyImmunohistochemistryInhibitionMacromolecular complexesNeurological diseasesNeuronsPathologyPharmacological targetsPotassium effluxSubcellular localizationG protein-gated inwardly rectifying K+ (GIRK/Kir3) channels are mainly expressed in excitable cells such as neurons and atrial myocytes, where they can respond to a wide variety of neurotransmitters. Four GIRK subunits have been found in mammals (GIRK1-4) and act as downstream targets for various Gai/o-linked G protein-coupled receptors (GPCRs). Activation of GIRK channels produces a postsynaptic efflux of potassium from the cell, responsible for hyperpolarization/inhibition of the neuron. A growing body of evidence suggests that dysregulation of GIRK signalling can lead to excessive or deficient neuronal excitability, which contributes to neurological diseases and disorders. Therefore, GIRK channels are proposed as new pharmacological targets. The function of GIRK channels in neurons is not only determined by their biophysical properties but also by their cellular and subcellular localization patterns and densities on the neuronal surface. GIRK channels can be located within several subcellular compartments, where they have many different functional implications. This subcellular localization changes dynamically along the neuronal surface in response to drug intake. Ongoing research is focusing on determining the proteins that form macromolecular complexes with GIRK channels and are responsible for fast and precise signalling under physiological conditions, and how their alteration is implicated in pathological conditions. In this review, the distinct regional, cellular, and subcellular distribution of GIRK channel subunits in the brain will be discussed in view of their possible functional and pathological implications.Sercrisma International S.L.202520252025info:eu-repo/semantics/articleapplication/pdfapplication/pdfhttps://www.hh.um.es/Abstracts/Vol_/_/__18822.htmhttps://hdl.handle.net/10578/42854reponame:RUIdeRA. Repositorio Institucional de la UCLMinstname:Universidad de Castilla-La ManchaInglésRTI2018-095812-B-I00PID2021-125875OB-I00MCIN/AEI/ 10.13039/501100011033SBPLY/17/180501/000229SBPLY/21/180501/0000642023-GRIN-34187info:eu-repo/semantics/openAccessoai:ruidera.uclm.es:10578/428542026-05-27T07:36:41Z
dc.title.none.fl_str_mv G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
title G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
spellingShingle G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
Martín Belmonte, Alejandro
G protein-coupled receptors (GPCRs)
GIRK channels
Hyperpolarization
Immunoelectron microscopy
Immunohistochemistry
Inhibition
Macromolecular complexes
Neurological diseases
Neurons
Pathology
Pharmacological targets
Potassium efflux
Subcellular localization
title_short G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
title_full G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
title_fullStr G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
title_full_unstemmed G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
title_sort G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels: Molecular, cellular, and subcellular diversity
dc.creator.none.fl_str_mv Martín Belmonte, Alejandro
Aguado Rubio, Carolina
Alfaro Ruiz, Rocío
Luján Miras, Rafael
author Martín Belmonte, Alejandro
author_facet Martín Belmonte, Alejandro
Aguado Rubio, Carolina
Alfaro Ruiz, Rocío
Luján Miras, Rafael
author_role author
author2 Aguado Rubio, Carolina
Alfaro Ruiz, Rocío
Luján Miras, Rafael
author2_role author
author
author
dc.subject.none.fl_str_mv G protein-coupled receptors (GPCRs)
GIRK channels
Hyperpolarization
Immunoelectron microscopy
Immunohistochemistry
Inhibition
Macromolecular complexes
Neurological diseases
Neurons
Pathology
Pharmacological targets
Potassium efflux
Subcellular localization
topic G protein-coupled receptors (GPCRs)
GIRK channels
Hyperpolarization
Immunoelectron microscopy
Immunohistochemistry
Inhibition
Macromolecular complexes
Neurological diseases
Neurons
Pathology
Pharmacological targets
Potassium efflux
Subcellular localization
description G protein-gated inwardly rectifying K+ (GIRK/Kir3) channels are mainly expressed in excitable cells such as neurons and atrial myocytes, where they can respond to a wide variety of neurotransmitters. Four GIRK subunits have been found in mammals (GIRK1-4) and act as downstream targets for various Gai/o-linked G protein-coupled receptors (GPCRs). Activation of GIRK channels produces a postsynaptic efflux of potassium from the cell, responsible for hyperpolarization/inhibition of the neuron. A growing body of evidence suggests that dysregulation of GIRK signalling can lead to excessive or deficient neuronal excitability, which contributes to neurological diseases and disorders. Therefore, GIRK channels are proposed as new pharmacological targets. The function of GIRK channels in neurons is not only determined by their biophysical properties but also by their cellular and subcellular localization patterns and densities on the neuronal surface. GIRK channels can be located within several subcellular compartments, where they have many different functional implications. This subcellular localization changes dynamically along the neuronal surface in response to drug intake. Ongoing research is focusing on determining the proteins that form macromolecular complexes with GIRK channels and are responsible for fast and precise signalling under physiological conditions, and how their alteration is implicated in pathological conditions. In this review, the distinct regional, cellular, and subcellular distribution of GIRK channel subunits in the brain will be discussed in view of their possible functional and pathological implications.
publishDate 2025
dc.date.none.fl_str_mv 2025
2025
2025
dc.type.none.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://www.hh.um.es/Abstracts/Vol_/_/__18822.htm
https://hdl.handle.net/10578/42854
url https://www.hh.um.es/Abstracts/Vol_/_/__18822.htm
https://hdl.handle.net/10578/42854
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv RTI2018-095812-B-I00
PID2021-125875OB-I00
MCIN/AEI/ 10.13039/501100011033
SBPLY/17/180501/000229
SBPLY/21/180501/000064
2023-GRIN-34187
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Sercrisma International S.L.
publisher.none.fl_str_mv Sercrisma International S.L.
dc.source.none.fl_str_mv reponame:RUIdeRA. Repositorio Institucional de la UCLM
instname:Universidad de Castilla-La Mancha
instname_str Universidad de Castilla-La Mancha
reponame_str RUIdeRA. Repositorio Institucional de la UCLM
collection RUIdeRA. Repositorio Institucional de la UCLM
repository.name.fl_str_mv
repository.mail.fl_str_mv
_version_ 1869404680330674176
score 15.811543

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