Gαi Controls the Gating of the G Protein-Activated K+ Channel, GIRK

Autor: Dalia Varon, Tatiana Ivanina, Sagit Peleg, Carmen W. Dessauer, Nathan Dascal
Rok vydání: 2002
Předmět:
medicine.medical_specialty
Potassium Channels
G protein
GTP-Binding Protein alpha Subunits
Neuroscience(all)
Gi alpha subunit
Alpha (ethology)
Down-Regulation
Gene Expression
Gating
GTP-Binding Protein alpha Subunits
Gi-Go

Synaptic Transmission
Membrane Potentials
Xenopus laevis
Internal medicine
Proto-Oncogene Proteins
medicine
Animals
G protein-coupled inwardly-rectifying potassium channel
RNA
Messenger

Potassium Channels
Inwardly Rectifying

Beta (finance)
Neurotransmitter Agents
Receptor
Muscarinic M2

Binding Sites
Chemistry
urogenital system
General Neuroscience
Immunohistochemistry
Receptors
Muscarinic

Cell biology
Protein Structure
Tertiary

G beta-gamma complex
Endocrinology
G Protein-Coupled Inwardly-Rectifying Potassium Channels
Guanosine 5'-O-(3-Thiotriphosphate)
Oocytes
Female
GTP-Binding Protein alpha Subunit
Gi2

Oligoribonucleotides
Antisense
Zdroj: Neuron. 33(1):87-99
ISSN: 0896-6273
DOI: 10.1016/s0896-6273(01)00567-0
Popis: GIRK (Kir3) channels are activated by neurotransmitters coupled to G proteins, via a direct binding of G(beta)(gamma). The role of G(alpha) subunits in GIRK gating is elusive. Here we demonstrate that G(alpha)(i) is not only a donor of G(beta)(gamma) but also regulates GIRK gating. When overexpressed in Xenopus oocytes, GIRK channels show excessive basal activity and poor activation by agonist or G(beta)(gamma). Coexpression of G(alpha)(i3) or G(alpha)(i1) restores the correct gating parameters. G(alpha)(i) acts neither as a pure G(beta)(gamma) scavenger nor as an allosteric cofactor for G(beta)(gamma). It inhibits only the basal activity without interfering with G(beta)(gamma)-induced response. Thus, GIRK is regulated, in distinct ways, by both arms of the G protein. G(alpha)(i) probably acts in its GDP bound form, alone or as a part of G(alpha)(beta)(gamma) heterotrimer.
Databáze: OpenAIRE