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Target intelligence / Profile preview
G protein-activated inward rectifier potassium channel 1 (GIRK1)
- Target
- GIRK1
- Molecular classification
- Ion channel, Potassium channel, Inward rectifier potassium channel, G protein-gated ion channel
01
Overview
G protein-activated inward rectifier potassium channel 1 (GIRK1) is a member of the inwardly rectifying potassium (Kir) channel family. GIRK channels are directly regulated by G proteins and play crucial roles in cellular excitability and signal transduction. They are activated via direct binding of G-protein βγ subunits released from GPCRs upon ligand stimulation and are involved in regulating electrical activity in the central nervous system and cardiac tissue. Dysfunction has been linked to several diseases including epilepsy, Down’s syndrome, Parkinson’s disease, drug addiction, as well as cardiac arrhythmias.
- Other names
- Kir3.1KCNJ3
02
Mechanism of action
Direct activation by G protein βγ subunits and PIP2, leading to potassium influx and hyperpolarization.
03
Biological functions
Regulation of membrane potentialRegulation of neuronal excitabilityRegulation of heart rateSignal transduction
04
Disease associations
EpilepsyDown’s syndromeParkinson’s diseaseDrug addictionCardiac arrhythmias
05
Safety considerations
Cardiac arrhythmias
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