Target intelligence / Profile preview

Glutamate ionotropic receptor kainate type subunit 3 (GRIK3)

Target
GRIK3
Molecular classification
Ion channel, Ligand-gated ion channel, Receptor
01

Overview

Glutamate ionotropic receptor kainate type subunit 3 (GRIK3, also known as GluK3 or GLUR7) is a subunit of the kainate family of ionotropic glutamate receptors. It forms tetrameric, cation-permeable, ligand-gated ion channels primarily responsive to glutamate and the agonist kainic acid. GRIK3 can form heteromeric receptors with other kainate subunits (such as GRIK4 or GRIK5), and is predominantly expressed in the brain, where it mediates fast excitatory neurotransmission at both pre- and postsynaptic sites. These receptors play a vital role in regulating synaptic transmission and plasticity, and their dysfunction is associated with a range of neurological and neuropsychiatric disorders including schizophrenia and autism spectrum disorder. GRIK3 activity is modulated by N-glycosylation and protein–protein interactions, and the receptor demonstrates unique gating and desensitization kinetics within its family. Drugs targeting GRIK3 may modulate synaptic excitability and are under investigation for their role in neurological disease.

Other names
GluK3GLUR7GluR7EAA5GluR-7GluR7aGLR7Glutamate receptor 7Excitatory amino acid receptor 5dJ1090M5.19630027E11
02

Mechanism of action

Kainate receptor agonists activate the cation channel, allowing influx of cations (Na+, Ca2+), leading to membrane depolarization and synaptic excitation. Antagonists bind the ligand binding domain to prevent channel opening.

03

Biological functions

Signal transductionSynaptic transmissionExcitatory neurotransmission
04

Disease associations

SchizophreniaAutism spectrum disorderNeurodegenerative diseaseEpilepsyOther neuropsychiatric disorders
05

Safety considerations

Overactivation may contribute to excitotoxicity and neuron damageMutations are implicated in neuropsychiatric disorders, possible adverse neurocognitive effects
06

Interacting drugs

Kainic acid

2 more in the full profile.

07

Biomarkers

Ser310Ala (S310A) polymorphism (studied in risk for schizophrenia)

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