Target intelligence / Profile preview

Glutamate receptor ionotropic, kainate 2 (GluK2)

Target
GluK2
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel, Ionotropic glutamate receptor
01

Overview

Glutamate receptor ionotropic, kainate 2 (GluK2) is a subunit of kainate receptors, which are tetrameric ligand-gated ion channels in the ionotropic glutamate receptor family. GluK2 assembles to form functional kainate receptors which mediate excitatory neurotransmission and modulate synaptic transmission and plasticity in the central nervous system. Kainate receptors, including those containing GluK2, are critical for normal synaptic signaling and are implicated in a range of neurological and psychiatric diseases due to their role in regulating neuronal circuits. The receptor can function as a homomer or as a heteromer with other kainate receptor subunits (GluK1–5), and its activation and desensitization are finely controlled by ligand binding and allosteric modulation.

Other names
GRIK2Kainate receptor subunit GluK2Ionotropic glutamate receptor kainate 2KA2GluR6
02

Mechanism of action

Agonists (e.g., glutamate, kainic acid, domoic acid) bind to the ligand-binding domain and open the cation-permeable channel, mediating excitatory currents. Positive allosteric modulators (e.g., BPAM344, concanavalin A) prolong activation by stabilizing the ligand-binding domain dimer and inhibiting desensitization.

03

Biological functions

Regulation of synaptic transmissionExcitatory neurotransmissionModulation of neuronal circuits and synaptic plasticity
04

Disease associations

Neurodegenerative disease (e.g., Alzheimer’s, Parkinson’s)EpilepsySchizophreniaDepressionAnxietyAutism spectrum disorder
05

Safety considerations

Overactivation can lead to neurotoxicity and excitotoxic cell death.Therapeutic target engagement bears a risk for seizures and neuropsychiatric side effects due to broad central nervous system roles.Lack of highly selective ligands challenges targeted pharmacology.
06

Interacting drugs

Kainic acid

5 more in the full profile.

07

Biomarkers

No established clinical biomarkers for patient selection or monitoring; expression in brain regions may serve as a research biomarker in neuropsychiatric or neurodegenerative diseases, but not in clinical use.

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